Tozasertib (VX-680)
别名: MK-0457 中文名称：陶扎色替
Tozasertib (VX-680)是一种pan-Aurora抑制剂，对Aurora A作用最强，无细胞试验中Kiapp为0.6 nM，而对Aurora B/Aurora C的作用较弱，对Aurora A选择性比其他55种激酶高100倍。唯二的例外是 Fms-related tyrosine kinase-3 (FLT-3) 和 BCR-ABL tyrosine kinase，也可被 Tozasertib 抑制，对应的Ki值均为30 nM和30 nM。Tozasertib 可诱导凋亡和自噬。Phase 2。
Tozasertib (VX-680) Chemical Structure
CAS: 639089-54-6
产品质控
批次：
纯度：
99.99%
99.99
Tozasertib (VX-680)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 |
|---|---|---|---|---|---|
| HeLa | Function assay | 10 to 1000 nM | 48 hrs | Inhibition of Aurora kinase B in human HeLa cells assessed as delay in mitotic arrest by accumulation of multinucleated cells with 4N/8N DNA content at 10 to 1000 nM after 48 hrs by propidium iodide staining-based FACS flow cytometric analysis | 23808327 |
| HCT116 | Antitumor assay | 50 mg/kg | 5 days | Antitumor activity against human HCT116 cells xenografted in athymic nu/nu mouse assessed as reduction in tumor size at 50 mg/kg, iv qd for 5 days per week for 2 weeks measured twice a week | 23808327 |
| HCT116 | Function assay | 100 nM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 100 nM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 |
| HCT116 | Function assay | 1 uM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 1 uM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 |
| HCT116 | Function assay | 1 uM | 3 hrs | Inhibition of Aurora B in human HCT116 cells assessed as reduction in histone H3 phosphorylation at Ser10 residue up to 1 uM after 3 hrs by Western blot analysis | 30143423 |
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cyclin B1 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cdc2 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HCT15 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT15 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=1.23μM | 30143423 | |
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=0.45μM | 30143423 | |
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as increase in nuclear area after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=1.06μM | 29437386 | |
| L929sA | Function assay | 24 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 24 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=1.02μM | 29437386 | |
| L929sA | Function assay | 0.5 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 0.5 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=0.98μM | 29437386 | |
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as reduction in cell growth after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=0.97μM | 29437386 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay, IC50=4.32μM | 29358147 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay, IC50=2.93μM | 29358147 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay, IC50=1.3μM | 29358147 | |
| A431 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A431 cells after 48 hrs by CCK8 assay, IC50=0.24μM | 29358147 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay, IC50=0.127μM | 29358147 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay, IC50=0.079μM | 29358147 | |
| U937 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human U937 cells after 48 hrs by CCK8 assay, IC50=0.036μM | 29358147 | |
| HCT8 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT8 cells after 48 hrs by MTT assay, IC50=44.6μM | 25812967 | |
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50=27.3μM | 25812967 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=19.4μM | 25812967 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B in human HeLa cells after 12 hrs by ELISA method, IC50=0.453μM | 25812967 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A in human HeLa cells after 12 hrs by ELISA method, IC50=0.261μM | 25812967 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=3.3μM | 24910766 | |
| NCI-N87 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=11.6μM | 24681066 | |
| SKBR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=9.99μM | 24681066 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=5.81μM | 24681066 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.32μM | 24681066 | |
| PANC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.13μM | 24681066 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=3.05μM | 24681066 | |
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=2.93μM | 24681066 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=1.3μM | 24681066 | |
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.4μM | 24681066 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.24μM | 24681066 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.127μM | 24681066 | |
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0791μM | 24681066 | |
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0382μM | 24681066 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.036μM | 24681066 | |
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0212μM | 24681066 | |
| HCT116 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT116 cells after 96 hrs by MTS assay, EC50=0.12μM | 23808327 | |
| sf9 | Function assay | 15 mins | Inhibition of GST-tagged Aurora kinase A catalytic domain (123 to 401 amino acids) (unknown origin) expressed in sf9 cells using tetra(LRRWSLG) as substrate preincubated for 15 mins prior to substrate addition measured after 90 mins by luminescence assay, IC50=0.02μM | 23808327 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=0.38μM | 22572580 | |
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay, IC50=0.3μM | 22572580 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells assessed as distinct polyploidy phenotype after 72 hrs, Activity=0.03μM | 19143567 | |
| HCT116 | Cytotoxicity assay | 10 to 14 days | Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.024μM | 19143567 | |
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot analysis | 30143423 | |
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot method | 30143423 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.013μM | 30502115 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.148μM | 30502115 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50=35.8μM | 30502115 | |
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, GI50=45.3μM | 30502115 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50=46.2μM | 30502115 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=35.8μM | 30728112 | |
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, IC50=45.3μM | 30728112 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50=46.2μM | 30728112 | |
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH 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 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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 | ||
| 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 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| NCI-H358 | Antiproliferative assay | Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant at | 28038940 | ||
| NCI-H23 | Antiproliferative assay | Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant at | 28038940 | ||
| Hela | Function assay | Inhibition of recombinant Aurora A kinase derived from human Hela cells using kemptide as substrate in presence of [c-32P]ATP, Ki=0.002μM | 27884697 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.12μM | 23808327 | ||
| HCT116 | Function assay | Inhibition of Aurora B kinase assessed as reduction in histone H3 phosphorylation in human HCT116 cells, IC50=0.055μM | 21802948 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.028μM | 21802948 | ||
| insect | Function assay | Inhibition of human recombinant His-tagged Aurora A kinase expressed in insect cells, IC50=0.0007μM | 21194953 | ||
| BA/F3 | Function assay | Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells, IC50=5μM | 20604564 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant, IC50=0.03μM | 20604564 | ||
| HeLa | Function assay | Inhibition of phosphotransferase activity of recombinant aurora A expressed in HeLa cells, Ki=0.002μM | 20573509 | ||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by MTS assay, IC50=0.12μM | 20550212 | ||
| COLO205 | Antiproliferative assay | Antiproliferative activity against human COLO205 cells by [3H]thymidine uptake assay, IC50=0.019μM | 19447622 | ||
| H29 | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human H29 cells, IC50=0.74μM | 18630890 | ||
| HCT | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human HCT cells, IC50=0.31μM | 18630890 | ||
| HCT | Function assay | Inhibition of Aurora A assessed as separation of centrosomes in human HCT cells, IC50=0.31μM | 18630890 | ||
| HCT | Function assay | Inhibition of Aurora A in human HCT cells assessed as loss of autophosphorylation of Aurora A, IC50=0.31μM | 18630890 | ||
| HT29 | Antiproliferative assay | Antiproliferative activity against human HT29 cells, IC50=0.15μM | 18630890 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.053μM | 18630890 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50=0.048μM | 18630890 | ||
| TE-5 | Growth Inhibition Assay | IC50=49.7118 μM | SANGRER | ||
| NCI-H345 | Growth Inhibition Assay | IC50=48.468 μM | SANGRER | ||
| TE-6 | Growth Inhibition Assay | IC50=48.446 μM | SANGRER | ||
| L-363 | Growth Inhibition Assay | IC50=46.881 μM | SANGRER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=46.4612 μM | SANGRER | ||
| LS-513 | Growth Inhibition Assay | IC50=45.9156 μM | SANGRER | ||
| COR-L88 | Growth Inhibition Assay | IC50=45.2778 μM | SANGRER | ||
| DG-75 | Growth Inhibition Assay | IC50=45.1577 μM | SANGRER | ||
| NCI-H1694 | Growth Inhibition Assay | IC50=44.9472 μM | SANGRER | ||
| GI-1 | Growth Inhibition Assay | IC50=42.9192 μM | SANGRER | ||
| BC-1 | Growth Inhibition Assay | IC50=42.6731 μM | SANGRER | ||
| KU812 | Growth Inhibition Assay | IC50=41.507 μM | SANGRER | ||
| GDM-1 | Growth Inhibition Assay | IC50=38.9116 μM | SANGRER | ||
| JAR | Growth Inhibition Assay | IC50=38.2449 μM | SANGRER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=38.1654 μM | SANGRER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=37.815 μM | SANGRER | ||
| ES3 | Growth Inhibition Assay | IC50=36.675 μM | SANGRER | ||
| HCC2157 | Growth Inhibition Assay | IC50=35.4619 μM | SANGRER | ||
| TE-441-T | Growth Inhibition Assay | IC50=34.6371 μM | SANGRER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=34.5456 μM | SANGRER | ||
| A253 | Growth Inhibition Assay | IC50=33.5852 μM | SANGRER | ||
| A704 | Growth Inhibition Assay | IC50=33.5538 μM | SANGRER | ||
| COLO-684 | Growth Inhibition Assay | IC50=32.6438 μM | SANGRER | ||
| RXF393 | Growth Inhibition Assay | IC50=32.497 μM | SANGRER | ||
| CHP-126 | Growth Inhibition Assay | IC50=31.1984 μM | SANGRER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=31.1702 μM | SANGRER | ||
| KNS-42 | Growth Inhibition Assay | IC50=30.8956 μM | SANGRER | ||
| Raji | Growth Inhibition Assay | IC50=30.5592 μM | SANGRER | ||
| SW962 | Growth Inhibition Assay | IC50=30.2747 μM | SANGRER | ||
| SNU-C1 | Growth Inhibition Assay | IC50=28.943 μM | SANGRER | ||
| U-266 | Growth Inhibition Assay | IC50=28.6366 μM | SANGRER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=28.6143 μM | SANGRER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=28.0734 μM | SANGRER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=27.5585 μM | SANGRER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=27.1773 μM | SANGRER | ||
| NCI-H748 | Growth Inhibition Assay | IC50=25.7627 μM | SANGRER | ||
| no-11 | Growth Inhibition Assay | IC50=25.747 μM | SANGRER | ||
| MPP-89 | Growth Inhibition Assay | IC50=25.5314 μM | SANGRER | ||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=25.4752 μM | SANGRER | ||
| REH | Growth Inhibition Assay | IC50=25.4671 μM | SANGRER | ||
| NCI-H889 | Growth Inhibition Assay | IC50=25.1931 μM | SANGRER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=25.1526 μM | SANGRER | ||
| KLE | Growth Inhibition Assay | IC50=22.1903 μM | SANGRER | ||
| BOKU | Growth Inhibition Assay | IC50=21.4533 μM | SANGRER | ||
| LP-1 | Growth Inhibition Assay | IC50=21.3432 μM | SANGRER | ||
| EVSA-T | Growth Inhibition Assay | IC50=21.1499 μM | SANGRER | ||
| CAL-148 | Growth Inhibition Assay | IC50=20.9934 μM | SANGRER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=19.8227 μM | SANGRER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=19.6663 μM | SANGRER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=19.555 μM | SANGRER | ||
| Calu-6 | Growth Inhibition Assay | IC50=19.239 μM | SANGRER | ||
| SF539 | Growth Inhibition Assay | IC50=17.9922 μM | SANGRER | ||
| HH | Growth Inhibition Assay | IC50=17.1963 μM | SANGRER | ||
| ES6 | Growth Inhibition Assay | IC50=16.2361 μM | SANGRER | ||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=15.6326 μM | SANGRER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=14.4433 μM | SANGRER | ||
| NCI-H1417 | Growth Inhibition Assay | IC50=14.3052 μM | SANGRER | ||
| LS-123 | Growth Inhibition Assay | IC50=14.1588 μM | SANGRER | ||
| CTB-1 | Growth Inhibition Assay | IC50=14.0329 μM | SANGRER | ||
| EW-3 | Growth Inhibition Assay | IC50=13.7402 μM | SANGRER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=13.5788 μM | SANGRER | ||
| NEC8 | Growth Inhibition Assay | IC50=13.1038 μM | SANGRER | ||
| HCE-T | Growth Inhibition Assay | IC50=13.0049 μM | SANGRER | ||
| LC4-1 | Growth Inhibition Assay | IC50=12.7706 μM | SANGRER | ||
| KG-1 | Growth Inhibition Assay | IC50=12.6545 μM | SANGRER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=12.4066 μM | SANGRER | ||
| A3-KAW | Growth Inhibition Assay | IC50=12.3236 μM | SANGRER | ||
| NB1 | Growth Inhibition Assay | IC50=12.29 μM | SANGRER | ||
| OPM-2 | Growth Inhibition Assay | IC50=12.1596 μM | SANGRER | ||
| DMS-153 | Growth Inhibition Assay | IC50=12.0426 μM | SANGRER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=11.9426 μM | SANGRER | ||
| NB69 | Growth Inhibition Assay | IC50=11.7705 μM | SANGRER | ||
| TALL-1 | Growth Inhibition Assay | IC50=11.4058 μM | SANGRER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=11.3827 μM | SANGRER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=11.2891 μM | SANGRER | ||
| NCCIT | Growth Inhibition Assay | IC50=11.0582 μM | SANGRER | ||
| SNB75 | Growth Inhibition Assay | IC50=10.076 μM | SANGRER | ||
| KY821 | Growth Inhibition Assay | IC50=9.77484 μM | SANGRER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=9.32844 μM | SANGRER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=8.90265 μM | SANGRER | ||
| KALS-1 | Growth Inhibition Assay | IC50=8.83851 μM | SANGRER | ||
| CP67-MEL | Growth Inhibition Assay | IC50=8.5326 μM | SANGRER | ||
| GCIY | Growth Inhibition Assay | IC50=8.36965 μM | SANGRER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=8.25637 μM | SANGRER | ||
| IA-LM | Growth Inhibition Assay | IC50=7.859 μM | SANGRER | ||
| NCI-H1436 | Growth Inhibition Assay | IC50=7.69932 μM | SANGRER | ||
| KM-H2 | Growth Inhibition Assay | IC50=7.18457 μM | SANGRER | ||
| UACC-257 | Growth Inhibition Assay | IC50=7.04512 μM | SANGRER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=6.78405 μM | SANGRER | ||
| LS-1034 | Growth Inhibition Assay | IC50=6.7566 μM | SANGRER | ||
| DJM-1 | Growth Inhibition Assay | IC50=6.34666 μM | SANGRER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=5.98597 μM | SANGRER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=5.81454 μM | SANGRER | ||
| Daudi | Growth Inhibition Assay | IC50=5.6912 μM | SANGRER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=5.64574 μM | SANGRER | ||
| TE-1 | Growth Inhibition Assay | IC50=5.49004 μM | SANGRER | ||
| TK10 | Growth Inhibition Assay | IC50=5.35469 μM | SANGRER | ||
| MC-CAR | Growth Inhibition Assay | IC50=5.06757 μM | SANGRER | ||
| SF268 | Growth Inhibition Assay | IC50=4.79916 μM | SANGRER | ||
| COR-L279 | Growth Inhibition Assay | IC50=4.75891 μM | SANGRER | ||
| HC-1 | Growth Inhibition Assay | IC50=4.69494 μM | SANGRER | ||
| LU-139 | Growth Inhibition Assay | IC50=4.61835 μM | SANGRER | ||
| TE-12 | Growth Inhibition Assay | IC50=4.56394 μM | SANGRER | ||
| SW872 | Growth Inhibition Assay | IC50=4.3434 μM | SANGRER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=4.22723 μM | SANGRER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=4.02467 μM | SANGRER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=3.9924 μM | SANGRER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=3.95312 μM | SANGRER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=3.94221 μM | SANGRER | ||
| ES1 | Growth Inhibition Assay | IC50=3.92293 μM | SANGRER | ||
| NCI-H2171 | Growth Inhibition Assay | IC50=3.92423 μM | SANGRER | ||
| NOS-1 | Growth Inhibition Assay | IC50=3.84754 μM | SANGRER | ||
| HEL | Growth Inhibition Assay | IC50=3.632 μM | SANGRER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=3.58603 μM | SANGRER | ||
| PF-382 | Growth Inhibition Assay | IC50=3.35778 μM | SANGRER | ||
| LOUCY | Growth Inhibition Assay | IC50=3.18693 μM | SANGRER | ||
| TE-9 | Growth Inhibition Assay | IC50=3.26736 μM | SANGRER | ||
| RH-1 | Growth Inhibition Assay | IC50=3.17291 μM | SANGRER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=3.02274 μM | SANGRER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=2.91253 μM | SANGRER | ||
| LU-134-A | Growth Inhibition Assay | IC50=2.8926 μM | SANGRER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=2.88126 μM | SANGRER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=2.86868 μM | SANGRER | ||
| NCI-H2107 | Growth Inhibition Assay | IC50=2.83711 μM | SANGRER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=2.83838 μM | SANGRER | ||
| TGW | Growth Inhibition Assay | IC50=2.65832 μM | SANGRER | ||
| ACN | Growth Inhibition Assay | IC50=2.50213 μM | SANGRER | ||
| K5 | Growth Inhibition Assay | IC50=2.40319 μM | SANGRER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.4613 μM | SANGRER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=2.29765 μM | SANGRER | ||
| SH-4 | Growth Inhibition Assay | IC50=2.32469 μM | SANGRER | ||
| NB17 | Growth Inhibition Assay | IC50=2.2927 μM | SANGRER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=2.06244 μM | SANGRER | ||
| RPMI-6666 | Growth Inhibition Assay | IC50=2.16207 μM | SANGRER | ||
| ATN-1 | Growth Inhibition Assay | IC50=2.02858 μM | SANGRER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.02654 μM | SANGRER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=1.97057 μM | SANGRER | ||
| GB-1 | Growth Inhibition Assay | IC50=2.01647 μM | SANGRER | ||
| A101D | Growth Inhibition Assay | IC50=1.87395 μM | SANGRER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.83073 μM | SANGRER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.78911 μM | SANGRER | ||
| TE-8 | Growth Inhibition Assay | IC50=1.80368 μM | SANGRER | ||
| NCI-H1963 | Growth Inhibition Assay | IC50=1.70583 μM | SANGRER | ||
| NB5 | Growth Inhibition Assay | IC50=1.64229 μM | SANGRER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=1.35405 μM | SANGRER | ||
| CMK | Growth Inhibition Assay | IC50=1.42117 μM | SANGRER | ||
| GT3TKB | Growth Inhibition Assay | IC50=1.28057 μM | SANGRER | ||
| DEL | Growth Inhibition Assay | IC50=1.25643 μM | SANGRER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.22212 μM | SANGRER | ||
| EW-1 | Growth Inhibition Assay | IC50=1.18562 μM | SANGRER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=1.21111 μM | SANGRER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=1.18005 μM | SANGRER | ||
| HAL-01 | Growth Inhibition Assay | IC50=1.16709 μM | SANGRER | ||
| ETK-1 | Growth Inhibition Assay | IC50=1.13613 μM | SANGRER | ||
| TE-10 | Growth Inhibition Assay | IC50=1.12946 μM | SANGRER | ||
| SBC-1 | Growth Inhibition Assay | IC50=1.12542 μM | SANGRER | ||
| HL-60 | Growth Inhibition Assay | IC50=1.06574 μM | SANGRER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.02775 μM | SANGRER | ||
| HCC1187 | Growth Inhibition Assay | IC50=1.00505 μM | SANGRER | ||
| DU-4475 | Growth Inhibition Assay | IC50=1.01756 μM | SANGRER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=0.96189 μM | SANGRER | ||
| SF126 | Growth Inhibition Assay | IC50=0.94819 μM | SANGRER | ||
| ES4 | Growth Inhibition Assay | IC50=0.91128 μM | SANGRER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.90259 μM | SANGRER | ||
| ALL-PO | Growth Inhibition Assay | IC50=0.88175 μM | SANGRER | ||
| KGN | Growth Inhibition Assay | IC50=0.89995 μM | SANGRER | ||
| HCE-4 | Growth Inhibition Assay | IC50=0.88063 μM | SANGRER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.86385 μM | SANGRER | ||
| HOP-62 | Growth Inhibition Assay | IC50=0.86329 μM | SANGRER | ||
| TE-15 | Growth Inhibition Assay | IC50=0.85098 μM | SANGRER | ||
| HCC1599 | Growth Inhibition Assay | IC50=0.80874 μM | SANGRER | ||
| MC116 | Growth Inhibition Assay | IC50=0.85011 μM | SANGRER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.7914 μM | SANGRER | ||
| NB6 | Growth Inhibition Assay | IC50=0.77254 μM | SANGRER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=0.71982 μM | SANGRER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.65346 μM | SANGRER | ||
| ONS-76 | Growth Inhibition Assay | IC50=0.66458 μM | SANGRER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.64403 μM | SANGRER | ||
| NCI-H187 | Growth Inhibition Assay | IC50=0.6413 μM | SANGRER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.63798 μM | SANGRER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.58773 μM | SANGRER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.63571 μM | SANGRER | ||
| LS-411N | Growth Inhibition Assay | IC50=0.57752 μM | SANGRER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=0.54392 μM | SANGRER | ||
| KE-37 | Growth Inhibition Assay | IC50=0.52102 μM | SANGRER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=0.43823 μM | SANGRER | ||
| NCI-H524 | Growth Inhibition Assay | IC50=0.51147 μM | SANGRER | ||
| K-562 | Growth Inhibition Assay | IC50=0.43472 μM | SANGRER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.42676 μM | SANGRER | ||
| RL95-2 | Growth Inhibition Assay | IC50=0.40567 μM | SANGRER | ||
| BL-70 | Growth Inhibition Assay | IC50=0.38974 μM | SANGRER | ||
| LXF-289 | Growth Inhibition Assay | IC50=0.40406 μM | SANGRER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=0.3813 μM | SANGRER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=0.37272 μM | SANGRER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.35178 μM | SANGRER | ||
| IMR-5 | Growth Inhibition Assay | IC50=0.3554 μM | SANGRER | ||
| A388 | Growth Inhibition Assay | IC50=0.34086 μM | SANGRER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=0.33781 μM | SANGRER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.33459 μM | SANGRER | ||
| RKO | Growth Inhibition Assay | IC50=0.30813 μM | SANGRER | ||
| CESS | Growth Inhibition Assay | IC50=0.31328 μM | SANGRER | ||
| NB13 | Growth Inhibition Assay | IC50=0.27984 μM | SANGRER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.26641 μM | SANGRER | ||
| MEG-01 | Growth Inhibition Assay | IC50=0.27849 μM | SANGRER | ||
| SR | Growth Inhibition Assay | IC50=0.24564 μM | SANGRER | ||
| KM12 | Growth Inhibition Assay | IC50=0.2636 μM | SANGRER | ||
| EW-16 | Growth Inhibition Assay | IC50=0.23768 μM | SANGRER | ||
| KS-1 | Growth Inhibition Assay | IC50=0.23785 μM | SANGRER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=0.23337 μM | SANGRER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=0.22591 μM | SANGRER | ||
| ST486 | Growth Inhibition Assay | IC50=0.23087 μM | SANGRER | ||
| PSN1 | Growth Inhibition Assay | IC50=0.22026 μM | SANGRER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.21523 μM | SANGRER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.20086 μM | SANGRER | ||
| SW982 | Growth Inhibition Assay | IC50=0.2138 μM | SANGRER | ||
| K052 | Growth Inhibition Assay | IC50=0.1948 μM | SANGRER | ||
| OCUB-M | Growth Inhibition Assay | IC50=0.16983 μM | SANGRER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=0.15965 μM | SANGRER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=0.16707 μM | SANGRER | ||
| TE-11 | Growth Inhibition Assay | IC50=0.14982 μM | SANGRER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.12641 μM | SANGRER | ||
| SW954 | Growth Inhibition Assay | IC50=0.12229 μM | SANGRER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=0.11563 μM | SANGRER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=0.08789 μM | SANGRER | ||
| BL-41 | Growth Inhibition Assay | IC50=0.10445 μM | SANGRER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.07879 μM | SANGRER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=0.07782 μM | SANGRER | ||
| ES8 | Growth Inhibition Assay | IC50=0.04613 μM | SANGRER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=0.05299 μM | SANGRER | ||
| NALM-6 | Growth Inhibition Assay | IC50=0.02552 μM | SANGRER | ||
| 697 | Growth Inhibition Assay | IC50=0.02471 μM | SANGRER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.01434 μM | SANGRER | ||
| MFH-ino | Growth Inhibition Assay | IC50=0.0099 μM | SANGRER | ||
| BE-13 | Growth Inhibition Assay | IC50=0.00338 μM | SANGRER | ||
| RS4-11 | Growth Inhibition Assay | IC50=0.00404 μM | SANGRER | ||
| Sf9 | Function assay | Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate, IC50=0.023μM | 30234987 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tozasertib (VX-680)是一种pan-Aurora抑制剂，对Aurora A作用最强，无细胞试验中Kiapp为0.6 nM，而对Aurora B/Aurora C的作用较弱，对Aurora A选择性比其他55种激酶高100倍。唯二的例外是 Fms-related tyrosine kinase-3 (FLT-3) 和 BCR-ABL tyrosine kinase，也可被 Tozasertib 抑制，对应的Ki值均为30 nM和30 nM。Tozasertib 可诱导凋亡和自噬。Phase 2。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 虽然VX-680具有多激酶特性，VX-680却诱导相似的细胞毒性，IC50约为300 nM，在G2/M期，核内复制期，及转染ABL或FLT-3激酶的BaF3细胞凋亡时，显示一个Aurora B 类似的抑制表现型。VX-680抑制CAL-62细胞增殖，这种作用存在时间依赖性。用VX-680处理14天，明显降低群体的数量和大小，处理8305C下降达到70%，处理CAL-62, 8505C,和BHT-101下降达到90%。用VX-680处理不同ATC细胞，抑制细胞增殖，IC50为25到150 nM，这种作用存在时间和剂量依赖性。在软琼脂中，VX-680明显削弱不同细胞系形成群落的能力。caspase-3的活性分析显示VX-680诱导不同细胞凋亡。VX-680处理CAL-62 细胞12小时，形成DNA含量≥4N细胞累积物。微速摄影分析显示VX-680处理的CAL-62细胞离开细胞中期。VX-680可以抑制组蛋白H3的磷酸化作用。[2] VX-680作用于携带T315I突变的BCR-Abl的病人样本，具有明显抑制活性。[3] | |||
|---|---|---|---|---|
| 激酶实验 | 激酶抑制实验 | |||
| 丙酮酸激酶/乳酸脱氢酶催化NADH的氧化，伴随着ATP的消耗，观察340 nm 处吸光值的降低。反应包括100 mM Tris (pH 为 8), 10 mM MgCl2, 2.2 mM ATP, 1 mM磷酸烯醇丙酮酸, 0.6 mg/ml NADH, 75 ml丙酮酸激酶, 105 ml 乳酸脱氢酶,和0.5 mM 基底肽(序列为EAIYAAPFAKKK)。加入足够的激酶开始反应，反应的激酶浓度达到30 nM，用微量滴定板分光光度计在30oC进行30分钟，观察吸收率的降低。通过加入3.75 μl 溶于100% DMSO的VX-680 或单独DMSO，获得抑制常数。按如下公式计算Ki值，Ki = IC50/(1+[S]/Kd),[S]=[ATP]=2.2 mM, Kd=70 μM。假定作用于野生型和H396P Abl 激酶域的Kd(ATP)为70 μM，计算以上各值。 | ||||
| 细胞实验 | 细胞系 | CAL-62细胞 | ||
| 浓度 | 5-500 nM | |||
| 孵育时间 | 4天 | |||
| 方法 | 对照组CAL-62细胞培养在二甲亚砜和DMSO中，实验组加入500 nM VX-680，处理1到5天。加入不同浓度(5到500 nM) Aurora抑制剂处理不同ATC细胞4天，用来测定VX-680作用于细胞增殖的剂量依赖性。细胞在温育结束前加30 mM BrdU标记，脉冲2小时。通过比色免疫分析使用细胞增殖ELISA试剂盒分析BrdU的合并率。通过比较VX-680处理的细胞和对照组细胞得到结果， |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | DLK / p-MKK7 / MKK7 / p-JNK / JNK p-AURKA / AURKA / Survivin YAP p-AKT / p-GSK3β / Cleaved caspase-3 / Cleaved PARP |
|
23431148 | |
| Immunofluorescence | α-tubulin / Aurora-A |
|
21600017 | |
| Growth inhibition assay | Cell viability |
|
21600017 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | VX-680作用于人类AML(HL-60)移植瘤模型明显降低肿瘤尺寸。VX-680按75 mg/kg剂量给药实验鼠,每天腹腔注射两次，持续13天,与对照组相比，平均肿瘤体积下降达98%。肿瘤体积比实验之前初始体积小很多。按12.5 mg/kg剂量每天给药两次，肿瘤生长也明显降低，这种作用存在剂量依赖性。VX-680耐受性很好，只有在使用高剂量时可以观察到实验动物体重稍微降低。通过比较cisplatin,按5.4 mg/kg剂量给药，每四天腹腔注射一次，一共进行三次，抑制肿瘤生长只达9%。VX-680作用于胰脏和结肠移植瘤，也引起肿瘤衰退。VX-680静脉注射给药携带HCT116肿瘤的实验鼠，显示很强的抗癌活性。使用高剂量VX-680(每小时2 mg/kg)处理，明显提高效果，比实验钱的初始肿瘤平均尺寸下降56%。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 右侧腋窝处皮下注射107 HL-60白血病细胞的雌性无胸腺NCr-nu鼠 |
| Dosages | 50 mg/kg, 75 mg/kg | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00290550 | Terminated | Carcinoma Non-Small-Cell Lung |
Merck Sharp & Dohme LLC |
June 2006 | Phase 2 |
| NCT00111683 | Completed | Chronic Myelogenous Leukemia in Blast Crisis|Lymphocytic Leukemia B Cell Acute|Myelodysplastic Syndromes|Myelogenous Leukemia Chronic |
Merck Sharp & Dohme LLC |
June 2005 | Phase 1 |
化学信息&溶解度
| 分子量 | 464.59 | 分子式 | C23H28N8OS |
| CAS号 | 639089-54-6 | SDF | Download Tozasertib (VX-680) SDF |
| Smiles | CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 93 mg/mL ( (200.17 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。
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