Entinostat (MS-275)
别名: SNDX-275 中文名称：恩替诺特
Entinostat (MS-275, SNDX-275)强烈抑制HDAC1和HDAC3，无细胞试验中IC50分别为0.51 μM和1.7 μM，抑制作用强于HDACs 4， 6， 8，和10。Entinostat可诱导自噬和凋亡。Phase 3。
Entinostat (MS-275) Chemical Structure
CAS: 209783-80-2
产品质控
批次：
纯度：
99.96%
99.96
常与Entinostat (MS-275)一起在实验中被使用的化合物
Entinostat和Vorinostat证明了潜伏感染的原代T细胞中激活了HIV的产生。
Entinostat和Exemestane可显着改善晚期激素受体阳性、HER2阴性乳腺癌的无进展生存期和总生存期。
Connolly RM, et al. J Clin Oncol. 2021 Oct 1;39(28):3171-3181.
Entinostat和Decitabine诱导J82、J82CisR和RT-112细胞凋亡，并诱导J82和RT-112细胞系细胞周期停滞。
Entinostat (MS-275)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| U937 | Function assay | 5 uM | 24 hrs | Increase in histone H3 acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis. | 17447750 |
| HCT116 | Function assay | 10 uM | 24 hrs | Inhibition of HDAC1 in human HCT116 cells assessed as induction of hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. | 20452226 |
| NB4 | Cell cycle arrest assay | 5 uM | 24 hrs | Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis. | 20491440 |
| NB4 | Function assay | 5 uM | 24 hrs | Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis. | 20491440 |
| epithelial cells | Function assay | 1 uM | 4, 6, and 8 days | Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in short circuit currents at 1 uM for 4, 6, and 8 days relative to control. | 19966789 |
| Hela | Function assay | 0.6 uM | 16 hrs | Inhibition of HDAC6 in human Hela cells assessed as increase in total lysine acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy. | 21696956 |
| U937 | Cell cycle arrest assay | 5 uM | 30 hrs | Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 5 uM after 30 hrs by propidium iodide staining based flow cytometry. | 21215647 |
| NB4 | Function assay | 5 uM | 24 hrs | Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis. | 20491440 |
| C127-LT | Function assay | 1 uM | 24 hrs | Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 1 uM after 24 hrs by fluorescence microscopy. | 26996372 |
| C127-LT | Function assay | 10 uM | 24 hrs | Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 10 uM after 24 hrs by fluorescence microscopy. | 26996372 |
| HCT116 | Function assay | 10 uM | 24 hrs | Inhibition of HDAC2 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. | 22321215 |
| HCT116 | Function assay | 10 uM | 24 hrs | Inhibition of HDAC1 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis. | 22321215 |
| HeLa | Function assay | 1 uM | 6 hrs | Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as increase in intracellular acetyl-histone H4 levels at 1 uM after 6 hrs by Western blot analysis. | 29787262 |
| MV4-11 | Apoptosis assay | 5 uM | 24 to 48 hrs | Induction of apoptosis in human MV4-11 cells at 5 uM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry. | 29738953 |
| MV4-11 | Function assay | 200 nM | 24 hrs | Inhibition of class 1 HDAC in human MV4-11 cells assessed as hyperacetylation of histone H3 at 200 nM after 24 hrs by Western blot analysis. | 29738953 |
| HL60 | Apoptosis assay | 5 uM | 48 hrs | Induction of apoptosis in human HL60 cells assessed as decrease in procaspase-3 level at 5 uM after 48 hrs by Western blot analysis. | 28415009 |
| HL60 | Apoptosis assay | 5 uM | 48 hrs | Induction of apoptosis in human HL60 cells assessed as increase in cleaved caspase-3 level at 5 uM after 48 hrs by Western blot analysis. | 28415009 |
| HL60 | Apoptosis assay | 5 uM | 48 hrs | Induction of apoptosis in human HL60 cells assessed as increase in cleaved PARP level at 5 uM after 48 hrs by Western blot analysis. | 28415009 |
| MV4-11 | Cell cycle arrest assay | 5 uM | 24 hrs | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. | 29589441 |
| HEL | Cell cycle arrest assay | 5 uM | 24 hrs | Cell cycle arrest in human HEL cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. | 29589441 |
| Jurkat | Cell cycle arrest assay | 5 uM | 24 hrs | Cell cycle arrest in human Jurkat cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method. | 29589441 |
| MV4-11 | Function assay | 5 uM | 24 hrs | Inhibition of class 1 HDAC in human MV4-11 cells assessed as induction of histone hyperacetylation at 5 uM after 24 hrs by Western blot method. | 29589441 |
| LNCAP | Function assay | 10 uM | 24 hrs | Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation at 10 uM measured after 24 hrs relative to control. | 27717544 |
| epithelial cells | Function assay | 5 uM | Inhibition of HDAC in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM. | 19966789 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. | 22705022 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.1 μM. | 22705022 | |
| SK-N-BE(2) | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50 = 0.33 μM. | 28511906 | |
| AGS | Antiproliferative assay | 72 hrs | Antiproliferative activity against human AGS cells after 72 hrs by MTT assay, IC50 = 0.34 μM. | 29787262 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay, IC50 = 0.35 μM. | 26613635 | |
| HEL | Function assay | 3 hrs | Inhibition of class 1 HDAC in HEL cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.43 μM. | 28511906 | |
| PC3 | Growth inhibition assay | 48 hrs | Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay, GI50 = 0.43 μM. | 28395150 | |
| HEL | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HEL cells after 72 hrs by MTT assay, IC50 = 0.44 μM. | 29787262 | |
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay, IC50 = 0.45 μM. | 29787262 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay, IC50 = 0.47 μM. | 29202397 | |
| HEL | Antiproliferative assay | 48 hrs | Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 0.48 μM. | 28511906 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells incubated for 72 hrs by MTT assay, IC50 = 0.55 μM. | 25953722 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.55 μM. | 25874326 | |
| HCT116 | Growth inhibition assay | 2 days | Growth inhibition of human HCT116 cells after 2 days by MTT assay, GI50 = 0.6 μM. | 22541394 | |
| HL60 | Function assay | 3 hrs | Inhibition of class 1 HDAC in human HL60 cells using Boc-Ac-Lys-AMC as substrate incubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.62 μM. | 28415009 | |
| MOLT4 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50 = 0.65 μM. | 28511906 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human P53 expressing HCT116 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 0.7 μM. | 19441846 | |
| HEK293T | Function assay | 1 hr | Inhibition of FLAG-tagged HDAC2 (unknown origin) expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 0.74 μM. | 29289885 | |
| HCT116 | Antiproliferative assay | 3 days | Antiproliferative activity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.76 μM. | 22321215 | |
| U937 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human U937 cells after 48 hrs by MTT assay, IC50 = 0.77 μM. | 28415009 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.78 μM. | 25874326 | |
| K562 | Function assay | 10 mins | Inhibition of KDAC3 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 0.79 μM. | 26681404 | |
| HCT116 | Cytotoxicity assay | 3 days | Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.8 μM. | 20452226 | |
| Sf9 | Function assay | 3 hrs | Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method, IC50 = 0.9 μM. | 28501514 | |
| HEK293T | Function assay | 1 hr | Inhibition of human FLAG-tagged HDAC1 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.07 μM. | 29289885 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human P53 expressing A549 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.2 μM. | 19441846 | |
| HEK293T | Function assay | 1 hr | Inhibition of human FLAG-tagged HDAC3 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.23 μM. | 29289885 | |
| HEL | Antiproliferative assay | 48 hrs | Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 1.29 μM. | 28415009 | |
| G401 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human G401 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.3 μM. | 19441846 | |
| Sf9 | Function assay | 3 hrs | Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins in presence of 0.2 uM SAHA by f, IC50 = 1.3 μM. | 28501514 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.32 μM. | 28511906 | |
| Huh7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50 = 1.4 μM. | 25490700 | |
| MDA-MB-231 | Growth inhibition assay | 48 hrs | Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.41 μM. | 28395150 | |
| K562 | Function assay | 10 mins | Inhibition of KDAC1 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 1.48 μM. | 26681404 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 1.52 μM. | 28415009 | |
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay, IC50 = 1.6 μM. | 29202397 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.68 μM. | 28415009 | |
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human P53-deficient HeLa cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.8 μM. | 19441846 | |
| HCT116 | Function assay | 18 hrs | Inhibition of HDAC in human HCT116 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 1.96 μM. | 28340413 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.03 μM. | 28340413 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.07 μM. | 28415009 | |
| NCI-H661 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H661 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 2.19 μM. | 25874326 | |
| NCI-H661 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H661 cells incubated for 72 hrs by MTT assay, IC50 = 2.19 μM. | 25953722 | |
| Sf9 | Function assay | 17 hrs | Inhibition of His6-tagged HDAC3/SMRT (395 to 489 residues) (unknown origin) co-expressed in baculovirus infected sf9 cells using (FAM)-labeled acetylated peptide substrate after 17 hrs by caliper microfluidic mobility shift assay, IC50 = 2.31206 μM. | 30179749 | |
| ACHN | Antiproliferative assay | 72 hrs | Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay, IC50 = 2.4 μM. | 29787262 | |
| SGC7901 | Growth inhibition assay | 72 hrs | Growth inhibition of human SGC7901 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 2.5 μM. | 23061376 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 2.55 μM. | 29787262 | |
| MDA-MB-231 | Anticancer assay | 72 hrs | Anticancer activity against human MDA-MB-231 cells after 72 hrs by MTT assay, GI = 2.8 μM. | 21741834 | |
| A2780 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A2780 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 3 μM. | 19441846 | |
| HCT116 | Anticancer assay | 72 hrs | Anticancer activity against human HCT116 cells after 72 hrs by MTT assay, GI = 3.1 μM. | 21741834 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 3.1 μM. | 29787262 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 3.11 μM. | 28340413 | |
| A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 3.134 μM. | 26140961 | |
| A2780 | Function assay | 18 hrs | Inhibition of HDAC in human A2780 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 3.15 μM. | 28340413 | |
| HeLa | Function assay | 30 mins | Inhibition of human HDAC in HeLa cells after 30 mins by Fluor de Lys fluorescence assay, IC50 = 3.2 μM. | 21889343 | |
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 3.66 μM. | 29787262 | |
| A375 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay, IC50 = 3.67 μM. | 29202397 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 4.02 μM. | 28340413 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 4.53 μM. | 28340413 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 4.63 μM. | 25874326 | |
| MGC803 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay, IC50 = 4.89 μM. | 29202397 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 4.89 μM. | 28511906 | |
| HuH7 | Cytotoxicity assay | 3 days | Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 5.1 μM. | 25490700 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 5.1 μM. | 26140961 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 5.41 μM. | 25874326 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay, IC50 = 5.41 μM. | 25953722 | |
| A2780 | Anticancer assay | 72 hrs | Anticancer activity against human A2780 cells after 72 hrs by MTT assay, GI = 5.7 μM. | 21741834 | |
| A549 | Growth inhibition assay | 48 hrs | Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay, GI50 = 5.76 μM. | 28395150 | |
| A2780 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay, IC50 = 5.89 μM. | 28340413 | |
| SMMC7721 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SMMC7721 cells after 72 hrs by CCK-8 assay, IC50 = 5.97 μM. | 29202397 | |
| U266 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human U266 cells after 48 hrs by MTT assay, IC50 = 6.1 μM. | 28415009 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 6.36 μM. | 28340413 | |
| U251 | Growth inhibition assay | 2 days | Growth inhibition of human U251 cells after 2 days by MTT assay, GI50 = 6.5 μM. | 22541394 | |
| NCI-H1299 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay, IC50 = 6.74 μM. | 29202397 | |
| AsPC1 | Growth inhibition assay | 48 hrs | Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay, GI50 = 6.9 μM. | 28395150 | |
| BGC823 | Growth inhibition assay | 72 hrs | Growth inhibition of human BGC823 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 7.1 μM. | 23061376 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 7.881 μM. | 26140961 | |
| DU145 | Anticancer assay | 72 hrs | Anticancer activity against human DU145 cells after 72 hrs by MTT assay, GI = 7.9 μM. | 21741834 | |
| Bel7402 | Growth inhibition assay | 72 hrs | Growth inhibition of human Bel7402 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8 μM. | 23061376 | |
| HeLa | Function assay | 20 mins | Inhibition of HDAC in human HeLa cells using fluor de Lys as substrate incubated for 20 mins by microplate spectrofluorometric analysis, IC50 = 8.02 μM. | 27060764 | |
| MGC803 | Growth inhibition assay | 72 hrs | Growth inhibition of human MGC803 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8.9 μM. | 23061376 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, GI50 = 9.32 μM. | 28629630 | |
| SMMC7721 | Growth inhibition assay | 72 hrs | Growth inhibition of human SMMC7721 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 11 μM. | 23061376 | |
| HeLa | Function assay | 24 to 48 hrs | Inhibition of HDAC in human HeLa cells using Boc-Lys(AC)-AMC as substrate after 24 to 48 hrs by spectrofluorometry, IC50 = 11.18 μM. | 26996372 | |
| SKHEP1 | Growth inhibition assay | 72 hrs | Growth inhibition of human SKHEP1 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 13 μM. | 23061376 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50 = 18.37 μM. | 28629630 | |
| PC3 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, GI50 = 19.09 μM. | 28629630 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50 = 19.24 μM. | 28629630 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, GI50 = 19.26 μM. | 28629630 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 27.47 μM. | 18701301 | |
| U251 | Growth inhibition assay | 2 days | Growth inhibition of human U251 cells after 2 days by MTT assay, TGI = 40 μM. | 22541394 | |
| HEK293 STF | Function assay | 24 hrs | Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay. | 19022675 | |
| A4-Fuk | Growth Inhibition Assay | IC50=1.15364 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=1.13165 μM | SANGER | ||
| LC-1F | Growth Inhibition Assay | IC50=1.12007 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=1.11513 μM | SANGER | ||
| L-540 | Growth Inhibition Assay | IC50=1.10604 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=1.07675 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=1.03454 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=1.0241 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=0.98959 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.97831 μM | SANGER | ||
| DMS-153 | Growth Inhibition Assay | IC50=0.97469 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=0.9683 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=0.96437 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=0.95901 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=0.95076 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=0.93284 μM | SANGER | ||
| EHEB | Growth Inhibition Assay | IC50=0.92585 μM | SANGER | ||
| GDM-1 | Growth Inhibition Assay | IC50=0.88687 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=0.88096 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=0.87917 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=0.87827 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=0.87171 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=0.85868 μM | SANGER | ||
| BL-70 | Growth Inhibition Assay | IC50=0.85702 μM | SANGER | ||
| LC4-1 | Growth Inhibition Assay | IC50=0.84007 μM | SANGER | ||
| CESS | Growth Inhibition Assay | IC50=0.81197 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=0.81084 μM | SANGER | ||
| CPC-N | Growth Inhibition Assay | IC50=0.80524 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=0.80147 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=0.7836 μM | SANGER | ||
| BC-3 | Growth Inhibition Assay | IC50=0.78308 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=0.77681 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.77567 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=0.77348 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=0.75999 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.74661 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=0.72617 μM | SANGER | ||
| COR-L279 | Growth Inhibition Assay | IC50=0.70996 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=0.70492 μM | SANGER | ||
| ECC12 | Growth Inhibition Assay | IC50=0.70086 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.68343 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=0.66817 μM | SANGER | ||
| SU-DHL-1 | Growth Inhibition Assay | IC50=0.65947 μM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=0.65794 μM | SANGER | ||
| NALM-6 | Growth Inhibition Assay | IC50=0.6486 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=0.64276 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=0.63541 μM | SANGER | ||
| LOUCY | Growth Inhibition Assay | IC50=0.63364 μM | SANGER | ||
| LU-165 | Growth Inhibition Assay | IC50=0.61812 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=0.60719 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=0.59825 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=0.58703 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=0.58504 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=0.58242 μM | SANGER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=0.57848 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=0.57073 μM | SANGER | ||
| BL-41 | Growth Inhibition Assay | IC50=0.56889 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=0.56657 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=0.56105 μM | SANGER | ||
| NCI-H524 | Growth Inhibition Assay | IC50=0.55401 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=0.55306 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=0.5438 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=0.54261 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=0.53663 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=0.53041 μM | SANGER | ||
| HCC1599 | Growth Inhibition Assay | IC50=0.5157 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=0.51028 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=0.50473 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=0.49661 μM | SANGER | ||
| NCI-H187 | Growth Inhibition Assay | IC50=0.49227 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=0.48358 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=0.47025 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=0.44501 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=0.43897 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=0.43453 μM | SANGER | ||
| BC-1 | Growth Inhibition Assay | IC50=0.43403 μM | SANGER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=0.43153 μM | SANGER | ||
| OPM-2 | Growth Inhibition Assay | IC50=0.41513 μM | SANGER | ||
| RPMI-6666 | Growth Inhibition Assay | IC50=0.4112 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=0.41017 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=0.40613 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=0.40367 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=0.40342 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=0.403 μM | SANGER | ||
| CHP-126 | Growth Inhibition Assay | IC50=0.40231 μM | SANGER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.39868 μM | SANGER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.38776 μM | SANGER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=0.38701 μM | SANGER | ||
| NCCIT | Growth Inhibition Assay | IC50=0.38649 μM | SANGER | ||
| ARH-77 | Growth Inhibition Assay | IC50=0.38193 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=0.37487 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.37121 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=0.36935 μM | SANGER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.3673 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=0.36022 μM | SANGER | ||
| CMK | Growth Inhibition Assay | IC50=0.35727 μM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=0.34261 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=0.3381 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=0.33716 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=0.3351 μM | SANGER | ||
| NB12 | Growth Inhibition Assay | IC50=0.31756 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=0.31348 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=0.30576 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.30256 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=0.28708 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.27833 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.24079 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=0.22959 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.20113 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.19619 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=0.19593 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=0.17627 μM | SANGER | ||
| CRO-AP2 | Growth Inhibition Assay | IC50=0.16889 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=0.13527 μM | SANGER | ||
| NCI-H1417 | Growth Inhibition Assay | IC50=0.12974 μM | SANGER | ||
| NCI-H1963 | Growth Inhibition Assay | IC50=0.11579 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=0.11255 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=0.10912 μM | SANGER | ||
| NCI-H748 | Growth Inhibition Assay | IC50=0.10334 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=0.09976 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=0.06355 μM | SANGER | ||
| SCC-3 | Growth Inhibition Assay | IC50=0.061 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=1.16641 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=1.16943 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=1.17659 μM | SANGER | ||
| NCI-H719 | Growth Inhibition Assay | IC50=1.17898 μM | SANGER | ||
| EVSA-T | Growth Inhibition Assay | IC50=1.18114 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=1.20266 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=1.21489 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=1.22118 μM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=1.23112 μM | SANGER | ||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=1.24721 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=1.24776 μM | SANGER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=1.26478 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=1.27425 μM | SANGER | ||
| NB1 | Growth Inhibition Assay | IC50=1.27732 μM | SANGER | ||
| NCI-H64 | Growth Inhibition Assay | IC50=1.28462 μM | SANGER | ||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=1.28577 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.28663 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=1.28866 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=1.29947 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=1.30998 μM | SANGER | ||
| CAL-148 | Growth Inhibition Assay | IC50=1.32542 μM | SANGER | ||
| NCI-H2171 | Growth Inhibition Assay | IC50=1.34502 μM | SANGER | ||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=1.3539 μM | SANGER | ||
| NCI-H2107 | Growth Inhibition Assay | IC50=1.35883 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=1.38978 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=1.39219 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=1.42287 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=1.42691 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=1.42741 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=1.43615 μM | SANGER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=1.45358 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=1.47103 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=1.47987 μM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=1.51764 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=1.51945 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=1.5226 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=1.53564 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=1.5667 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=1.5682 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=1.60144 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=1.61901 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=1.63406 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=1.63459 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=1.647 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=1.65677 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=1.68281 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=1.69605 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=1.70353 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=1.75234 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.77207 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=1.78879 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=1.79388 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=1.79508 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=1.80302 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=1.81395 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=1.83108 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=1.83563 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=1.84422 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=1.88234 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=1.89373 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=1.9272 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=1.9328 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=1.93866 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=2.00262 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=2.01966 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=2.04502 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=2.05124 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=2.10454 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=2.11482 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=2.11792 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=2.16873 μM | SANGER | ||
| NCI-H1522 | Growth Inhibition Assay | IC50=2.21723 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=2.26902 μM | SANGER | ||
| DG-75 | Growth Inhibition Assay | IC50=2.27148 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=2.32855 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=2.33094 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=2.33145 μM | SANGER | ||
| NCI-H345 | Growth Inhibition Assay | IC50=2.33277 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=2.34936 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=2.41092 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=2.42267 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=2.4777 μM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=2.48521 μM | SANGER | ||
| DMS-79 | Growth Inhibition Assay | IC50=2.54103 μM | SANGER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=2.67562 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=2.76876 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=2.77083 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=2.84823 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=2.85641 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=2.87711 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=2.9248 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=2.92957 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=3.00511 μM | SANGER | ||
| NCI-H2227 | Growth Inhibition Assay | IC50=3.02079 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=3.03513 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=3.05206 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=3.05376 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=3.14378 μM | SANGER | ||
| NCI-H2141 | Growth Inhibition Assay | IC50=3.16566 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=3.18279 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=3.21342 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=3.43659 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=3.45227 μM | SANGER | ||
| MFH-ino | Growth Inhibition Assay | IC50=3.46589 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=3.48174 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=3.51699 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=3.55563 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=3.59899 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=3.61624 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=3.62671 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=3.70947 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=3.77189 μM | SANGER | ||
| ECC4 | Growth Inhibition Assay | IC50=3.97195 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=3.97547 μM | SANGER | ||
| EB-3 | Growth Inhibition Assay | IC50=3.99633 μM | SANGER | ||
| SHP-77 | Growth Inhibition Assay | IC50=4.00524 μM | SANGER | ||
| NCI-H2196 | Growth Inhibition Assay | IC50=4.05625 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=4.06399 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=4.1087 μM | SANGER | ||
| NCI-H1694 | Growth Inhibition Assay | IC50=4.13405 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=4.15332 μM | SANGER | ||
| NCI-H1436 | Growth Inhibition Assay | IC50=4.18333 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=4.31432 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=4.33268 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=4.37312 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=4.89657 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=5.00416 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=5.13778 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=5.14112 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=5.38814 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=5.76343 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=5.90694 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=5.99494 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=6.08895 μM | SANGER | ||
| EW-24 | Growth Inhibition Assay | IC50=6.2851 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=6.42623 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=6.46321 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=6.67557 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=6.92301 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=8.13166 μM | SANGER | ||
| COLO-668 | Growth Inhibition Assay | IC50=8.27786 μM | SANGER | ||
| EW-12 | Growth Inhibition Assay | IC50=8.40803 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=8.84661 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=8.89319 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=8.99042 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=9.17746 μM | SANGER | ||
| WSU-NHL | Growth Inhibition Assay | IC50=9.77478 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=9.97904 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=10.2834 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=10.5924 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=11.6004 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=11.7682 μM | SANGER | ||
| NCI-H2081 | Growth Inhibition Assay | IC50=11.7786 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=12.2463 μM | SANGER | ||
| CAS-1 | Growth Inhibition Assay | IC50=12.3631 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=12.6131 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=12.7952 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=12.8013 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=14.3975 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=14.448 μM | SANGER | ||
| Raji | Growth Inhibition Assay | IC50=14.5049 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=14.6271 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=14.9696 μM | SANGER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=15.4633 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=17.7831 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=19.0186 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=20.6703 μM | SANGER | ||
| U-698-M | Growth Inhibition Assay | IC50=20.7075 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=20.7223 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=21.1716 μM | SANGER | ||
| NCI-H716 | Growth Inhibition Assay | IC50=21.3154 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=21.4133 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=22.4148 μM | SANGER | ||
| CA46 | Growth Inhibition Assay | IC50=31.6936 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=33.6503 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=35.9624 μM | SANGER | ||
| TUR | Growth Inhibition Assay | IC50=36.0521 μM | SANGER | ||
| REH | Growth Inhibition Assay | IC50=37.8211 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=42.2885 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=42.7853 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=43.1339 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=44.8218 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=47.5812 μM | SANGER | ||
| HepG2 | Function assay | Inhibition of human HepG2 cells, IC50 = 0.0009 μM. | 18247554 | ||
| HEK293 | Function assay | Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells, IC50 = 0.12 μM. | 19441846 | ||
| HEK293 | Function assay | Inhibition of HDAC1 in HEK293 cells, IC50 = 0.12 μM. | 18308563 | ||
| SNU16 | Function assay | Inhibition of HDAC from human SNU16 cells, IC50 = 0.233 μM. | 18247554 | ||
| HEK293 | Function assay | Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells, IC50 = 0.25 μM. | 19441846 | ||
| U937 | Function assay | Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay, IC50 = 0.3 μM. | 18381238 | ||
| HEK293 | Function assay | Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells, IC50 = 0.4 μM. | 19441846 | ||
| HEK293 | Function assay | Inhibition of HDAC3 in HEK293 cells, IC50 = 0.4 μM. | 18308563 | ||
| HCT116 | Function assay | Inhibition of human HCT116 cells, IC50 = 0.5 μM. | 18247554 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50 = 0.67 μM. | 21742496 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50 = 0.67 μM. | 21650221 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells by CellTiter-Blue cell viability assay, IC50 = 0.7 μM. | 18370373 | ||
| ML1 | Antitumor assay | Antitumor activity against mouse ML1 cells, IC50 = 0.75 μM. | 19534534 | ||
| SKBR3 | Antiproliferative assay | Antiproliferative activity against human SKBR3 cells, IC50 = 0.87 μM. | 18247554 | ||
| S2 | Function assay | Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells, IC50 = 0.94 μM. | 19317450 | ||
| A549 | Antiproliferative assay | Antiproliferative activity against human A549 cells by CellTiter-Blue cell viability assay, IC50 = 1.2 μM. | 18370373 | ||
| G401 | Antiproliferative assay | Antiproliferative activity against human G401 cells by CellTiter-Blue cell viability assay, IC50 = 1.3 μM. | 18370373 | ||
| HeLa | Antiproliferative assay | Antiproliferative activity against HeLa cells by alamar blue assay, IC50 = 1.58489 μM. | 17606370 | ||
| HeLa | Antiproliferative assay | Antiproliferative activity against human HeLa cells by CellTiter-Blue cell viability assay, IC50 = 1.8 μM. | 18370373 | ||
| DU145 | Cytotoxicity assay | Cytotoxicity against human DU145 cells by MTT assay, IC50 = 2 μM. | 19131248 | ||
| K562 | Function assay | Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells., IC50 = 2 μM. | 12419380 | ||
| K562 | Function assay | Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells, IC50 = 2 μM. | 14592473 | ||
| SNU-16 | Function assay | Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells, IC50 = 2.19459 μM. | 14667227 | ||
| A2780 | Antiproliferative assay | Antiproliferative activity against human A2780 cells by CellTiter-Blue cell viability assay, IC50 = 3 μM. | 18370373 | ||
| SW620 | Function assay | Inhibition of human SW620 cells, IC50 = 3.2 μM. | 18247554 | ||
| A549 | Antiproliferative assay | Antiproliferative activity against human A549 cells, IC50 = 3.58 μM. | 18247554 | ||
| MKN45 | Antiproliferative assay | Antiproliferative activity against human MKN45 cells, IC50 = 4.16 μM. | 18247554 | ||
| MCF7 | Function assay | Inhibition of human MCF7 cells, IC50 = 4.3 μM. | 18247554 | ||
| K562 | Function assay | Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells., IC50 = 4.8 μM. | 10425110 | ||
| HeLa | Function assay | Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation, IC50 = 4.8 μM. | 19534534 | ||
| HeLa | Function assay | Inhibition of HDAC in HeLa cells, IC50 = 12.5892 μM. | 17606370 | ||
| U937 | Function assay | Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay. | 18381238 | ||
| U937 | Function assay | Induction of histone H4 hyperacetylation in human U937 cells. | 18381238 | ||
| U937 | Function assay | Inhibition of human HDAC4 in U937 cells by immunoprecipitation assay. | 18381238 | ||
| U937 | Function assay | Induction of granulocytic differentiation in human U937 cells. | 18381238 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells. | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells. | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells. | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells. | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells. | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells. | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells. | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells. | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells. | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells. | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells. | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells. | 29435139 | ||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells. | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells. | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells. | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells. | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells. | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells. | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells). | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells. | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells. | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells. | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells. | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells. | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells. | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells. | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells. | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells. | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells. | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells. | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells. | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells. | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells. | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells. | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells. | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells. | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells. | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Entinostat (MS-275, SNDX-275)强烈抑制HDAC1和HDAC3，无细胞试验中IC50分别为0.51 μM和1.7 μM，抑制作用强于HDACs 4， 6， 8，和10。Entinostat可诱导自噬和凋亡。Phase 3。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | MS-275通过作用于2′-氨基而抑制HDACs。MS-275作用于 K562细胞，诱导 p21WAF1/CIP1和凝溶胶蛋白的累积。MS-275作用于A2780细胞，可以降低S期细胞，提高G1期细胞。 MS-275通过抑制HAD而抑制人类肿瘤细胞系，包括 A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St和 HCT-15细胞增殖， IC50 为41.5 nM到4.71 μM。[1]MS-275抑制HDACs，作用于HDAC1和 HDAC3时IC50 分别为0.51 μM和1.7 μM。而对其他的HDACs没有抑制效果，如HDAC4, 6, 8和10。[2]MS-275有效抑制人类白血病和淋巴癌细胞，包括U937, HL-60, K562, 和Jurkat。MS-275可以诱导U937细胞p21CIP1/WAF1 调节的生长和变异Marker (CD11b)的表达。MS-275降低cyclin D1和抗凋亡蛋白Mcl-1与XIAP的表达。[3] | |||
|---|---|---|---|---|
| 激酶实验 | 标准HDAC实验 | |||
| 用HDAC buffer按1:6稀释鼠肝内的酶。重组人类HDACs按1:4稀释在HDAC buffer中。用于标准HDAC实验，60 μl HDAC buffer和10 μl 稀释的酶溶液在30oC混合。在HDAC buffer中加入30 μl基底液开始HDAC反应，随后在30oC下温育30分钟。加入100 μl胰蛋白酶溶液终止反应，胰蛋白酶溶液由溶于50 mM Tris-HCl（pH 为8.0）的10 mg/ml 胰蛋白酶, 100 mM NaCl,及 2 μM TSA组成。30oC下温育20分钟， 通过测定460纳米(λex = 390 nm)处的荧光监测AMC的释放。使用释放的AMC校准荧光强度 。用于标准时间过程实验，在初始100 μl HDAC 反应中加入20 pmol 基底物。2-50 pmol 基底物的酶法分析产物获得荧光AMC，通过测量这种荧光AMC来测定 Km值和 Vmax值。使用Hanes 图分析实验数据。记录的AMC信号是针对没有酶而有buffer和基底物的空白区。 | ||||
| 细胞实验 | 细胞系 | A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St和HCT-15细胞 | ||
| 浓度 | 10 μM 左右 | |||
| 孵育时间 | 3天 | |||
| 方法 | 5×103个肿瘤细胞接种到96孔板上，加入梯度浓度MS-275培养三天。细胞用0.1 mg/mL中性红在CO2反应器中染色1小时，测定中性红与50 μL乙醇和150 μL 0.1 M Na2HPO4溶解后的OD540,测定IC50值。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3 Cleaved PARP Caspase 8 DR4 / DR5 TopoIIα / TopoIIβ |
|
24203492 | |
| Immunofluorescence | phalloidin / snail DR4 / DR5 H3K4Me3 / H3K9Me3 |
|
29855565 | |
| Growth inhibition assay | Cell proliferation Cell viability |
|
24203492 | |
| ELISA | GCP-2 / MCP-2 / MIF |
|
24241152 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | MS-275按49 mg/kg剂量作用于除了HCT-15的人类移植瘤都显示出强抗癌活性。[1]MS-275促进恶性实体瘤和恶性血液病的治疗可能性，及生理和畸变基因表达的调节。[4]MS-275和IL-2联用，作用于肾细胞癌显示出强抗癌活性，因为降低调节性T细胞和增强脾细胞的表达。[5] | |
|---|---|---|
| 动物实验 | Animal Models | 侧腹皮下注射A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1和Calu-3细胞的裸鼠 |
| Dosages | 12.3, 24.5和49 mg/kg | |
| Administration | 每天口服处理一次，每周进行5天，持续4周。 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04708470 | Recruiting | Oropharyngeal Cancer|Neck Cancer|Human Papillomavirus|HPV|Anal Cancer|Cervical Cancer|Penile Cancer|Vulvar Cancer|Vaginal Cancer|Colon Cancer |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
October 5 2021 | Phase 1|Phase 2 |
| NCT03829930 | Terminated | Prostate Adenocarcinoma |
George Washington University |
May 1 2019 | Phase 1 |
| NCT03765229 | Completed | Melanoma |
UNC Lineberger Comprehensive Cancer Center|Syndax Pharmaceuticals |
March 22 2019 | Phase 2 |
| NCT03473639 | Completed | Metastatic Breast Cancer|Breast Cancer |
University of Virginia|Syndax Pharmaceuticals |
January 29 2019 | Phase 1 |
化学信息&溶解度
| 分子量 | 376.41 | 分子式 | C21H20N4O3 |
| CAS号 | 209783-80-2 | SDF | Download Entinostat (MS-275) SDF |
| Smiles | C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 75 mg/mL ( (199.25 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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* 必填项
常见问题及建议解决方法
问题 1:
I would like to use Entinostat（Catalog No.S1053） for animal study. What is your recommendation for the solvent? What is the role of PEG 300 in this case? Can I use DMSO only and dilute it with PBS or HBSS?
回答：
2%DMSO/30%PEG/68%Water is recommended. PEG is an important polymer that helps with the solubility of hydrophobic drugs. If you use DMSO only and dilute it with PBS or HBSS, Entinostat will likely to precipitate out since it has very low solubility in water.
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