FGFR
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
FGFR产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1490 |
Ponatinib (AP24534)Ponatinib (AP24534)是一种新型有效的多靶点抑制剂，在无细胞试验中作用于Abl，PDGFRα，VEGFR2，FGFR1和Src，IC50分别为0.37 nM，1.1 nM，1.5 nM，2.2 nM和5.4 nM。 |
RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
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| S2183 |
BGJ398 (NVP-BGJ398|Infigratinib)BGJ398 (NVP-BGJ398)是一种有效的，选择性FGFR抑制剂，作用于FGFR1/2/3，在无细胞试验中IC50为0.9 nM/1.4 nM/1 nM，作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上，对Abl， Fyn， Kit， Lck， Lyn和Yes几乎没有抑制活性。Phase 2。 |
Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIN3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 µM BGJ398, and 0.2 and 1 µM PD173074 were immunoblotted with the relevant antibodies. β-actin was used as a loading control. |
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| S1010 |
Nintedanib (BIBF 1120)Nintedanib (BIBF 1120) 尼达尼布是一种有效的三重血管激酶抑制剂，作用于VEGFR1/2/3， FGFR1/2/3和PDGFRα/β，在无细胞试验中IC50分别为34 nM/13 nM/13 nM， 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。 |
Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group |
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| S1264 |
PD173074PD173074是一种有效的FGFR1抑制剂，在无细胞试验中IC50约为25 nM，也能抑制VEGFR2，IC50为100-200 nM，作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。 |
FGFR inhibitors block signaling in FGFR2-fusion-expressing cells. Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIH3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 uM BGJ398, and 0.2 and 1 uM PD173074 were immunoblotted with the relevant antibodies. β-Actin was used as a loading control.
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| S1018 |
Dovitinib (TKI-258, CHIR-258)Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂，在无细胞试验中对III型(FLT3/c-Kit)作用最强，IC50为1 nM/2 nM，同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs，IC50为8-13 nM，但对InsR，EGFR，c-Met，EphA2，Tie2，IGF-1R和HER2作用较弱。Phase 4。 |
Orthotopic xenografts of HNSCC cell lines (A) SCC-1 and (B) OSC-19 were treated with dovitinib (20 mg/kg/day). In addition, the OSC-19 xenografts were treated with +/ radiation therapy. Marker, mean for triplicate; bars, SE. Statistical significance by unpaired t-test, p < 0.05. |
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| S8754New |
Alofanib(RPT835)Alofanib(RPT835)是一种新型的、选择性FGFR2变构抑制剂，在KATO III细胞中对FGF2诱导的FRS2α磷酸化具有显著的抑制效果，IC50小于10 nM。在细胞中，它对依赖于FGF2的FGFR1和FGFR3磷酸化水平没有直接作用，对FGF2-FGFR2的结合没有影响。 |
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| s9031New |
Gambogenic acidGambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. |
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| S8609New |
Derazantinib(ARQ-087)Derazantinib(ARQ-087)是具有口服生物活性的FGFR抑制剂，对FGFR2、FGFR1、FGFR3的IC50分别为1.8 nM、4.5 nM和4.5 nM，对FGFR4的抑制活性较低，IC50为34 nM。它还能抑制RET、DDR2、PDGFRβ、VEGFR和KIT。 |
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| S5234New |
Nintedanib Ethanesulfonate SaltNintedanib is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. |
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| S2801 |
AZD4547AZD4547是一种新型选择性的FGFR抑制剂，靶向作用于FGFR1/2/3，在无细胞试验中IC50为0.2 nM/2.5 nM/1.8 nM，对FGFR4， VEGFR2(KDR)具有微弱的作用活性，对IGFR， CDK2和p38几乎没有作用活性。Phase 2/3。 |
FCM evaluating lung CD11b+/Gr1+ myeloid cells isolated from 4T1 tumor-bearing mice after 20 days of treatment with AZD4547 or control. Statistical significance was assessed by unpaired t test. |
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| S1107 |
Danusertib (PHA-739358)Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Phase 2。 |
Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
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| S1084 |
Brivanib (BMS-540215)Brivanib (BMS-540215)是一种ATP竞争性的VEGFR2抑制剂，IC50为25 nM，对VEGFR-1和FGFR-1抑制作用适中，但比作用于PDGFR-β效果强240多倍。Phase 3。 |
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of Brivanib by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
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| S2769 |
Dovitinib (TKI-258) Dilactic AcidDovitinib (TKI-258) Dilactic Acid 是一种多靶点的RTK抑制剂，作用于III型(FLT3/c-Kit)最有效，IC50为1 nM/2 nM，也有效作用于IV型(FGFR1/3)和V型(VEGFR1-4)RTKs，IC50为8-13 nM，对InsR， EGFR， c-Met， EphA2， Tie2， IGFR1和HER2作用效果稍弱。Phase 4。 |
In vitro assays on CUX1-FGFR1-expressing Ba/F3 cells. a. IL-3 deprivation of Ba/F3 cells transduced with CUX1-FGFR1 resulted in transformation to growth factor independent growth. The mean growth ±SEM of three separate measurements over four consecutive days is presented. b. The dose-response curves of CUX1-FGFR1-transduced Ba/F3 cells, treated with TKI258 and PKC412 for 48 hours in the absence or presence of IL-3 (2 ng/ml) are presented. Points represent the average results of two experiments done in triplicate plotted with the curve-fitting GraphPad Prism 5 software; bars, SD. The calculated IC50 for each inhibitor is indicated. c. Western blot analyses of CUX1-FGFR1-transformed Ba/F3 cells after treatment with PKC412 and TKI258. Phosphorylation of CUX1-FGFR1 and its downstream effectors STAT5 and RPS6K decreased with increasing inhibitor concentrations. Expression of total CUX1-FGFR1, STAT5 and RPS6K remained unaffected. d. Effect of PKC412 and TKI258 on apoptosis of CUX1-FGFR1-expressing Ba/F3 cells after treatment for 48 hours. The percentage of apoptotic plus necrotic CUX1-FGFR1-transduced Ba/F3 cells is indicated.
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| S2774 |
MK-2461MK-2461是一种有效的，多靶点抑制剂，作用于c-Met(WT/mutants)，IC50为0.4-2.5 nM，对Ron，和Flt1作用效果稍弱；作用于c-Met比作用于FGFR1， FGFR2， FGFR3， PDGFRβ， KDR， Flt3， Flt4， TrkA和TrkB选择性高8到30倍。Phase 1/2。 |
Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
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| S1138 |
Brivanib Alaninate (BMS-582664)Brivanib Alaninate (BMS-582664)是BMS-540215的前体药物，是一种ATP竞争性的VEGFR2抑制剂，IC50为25 nM。 |
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| S7167 |
SSR128129ESSR128129E是口服效果较好的变构FGFR抑制剂，IC50为1.9μM，对别的关联RTKs无效果。 |
Western blot analysis of the expression and activation status (a) of pFGFR, pERK and Bim after treatment of API5-overexpressing cells (a) with either DMSO or SSR128129E.
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| S7057 |
LY2874455LY2874455是一个泛FGFR的抑制剂，对FGFR1，FGFR2, FGFR3, 和FGFR4的IC50值分别为2.8 nM, 2.6 nM, 6.4 nM,以及6 nM。并且也能抑制VEGFR2的活性，IC50为7 nM。Phase 1。 |
A: Overall structure of LY2874455/FGFR4 complex. B: The diagram of LY2874455. C: Fo-Fc omit map of LY2874455 in the FGFR4/LY2874455 complex. The electron density is superimposed with the final model. D: The DFG motif conformation of FGFR4. Active ApoFGFR4 DFG-in conformation is shown in blue (PDB: 4QQT); FGFR4/Ponatinib DFG-out conformation is shown in yellow (PDB: 4UXQ); FGFR4/BLU9931 DFG-in conformation is shown in pink (PDB: 4XCU); FGFR4/LY2874455 DFG-in conformation is shown in grey (this work). LY2874455 is highlighted in brown.
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| S7667 |
SU5402SU5402是一种有效的多靶点受体激酶抑制剂，对VEGFR2，FGFR1，和PDGF-Rβ的IC50分别为20 nM，30 nM，和510 nM。 |
Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.
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| S7765 |
Dovitinib (TKI258) LactateDovitinib (TKI258) Lactate是Dovitinib的乳酸盐，Dovitinib是一种多靶点的PTK抑制剂，主要对第III类(FLT3/c-Kit)发挥作用，IC50为1 nM/2 nM，对第IV 类(FGFR1/3)和第V 类(VEGFR1-4) RTKs也有效，IC50为8-13 nM，对InsR，EGFR，c-Met，EphA2，Tie2，IGFR1 和HER2作用较差。Phase 4。 |
(c) Percent survival for the AGS cancer cell line is shown with FGFR2 inhibitors of varying specificity. (d) The KatoIII diffuse gastric cancer cell line was treated with FGFR2 inhibitors of varying specificity. The Y-axis depicts percent survival versus the X-axis with log concentrations. In all panels, error bars represent standard error of the mean. The difference in percent cell survival between KatoIII and AGS cells was statistically significant (P <0.05) at the three highest concentrations of all drugs, except Brivanib which was only significant at the highest concentration. |
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| S8675 |
H3B-6527H3B-6527是一个高度选择性的共价FGFR4抑制剂，IC50 < 1.2 nM，其对FGFR4的选择性是对FGFR1-3选择性的250倍以上（对FGFR1-3的IC50s分别为320, 1290和1060 nM）。 |
KYSE150 and KYSE450 cells were treated each day with 1 μM H3B‐6527 or left untreated for three days, and lysates were immunoblotted with indicated antibodies. Western blotting demonstrated that the expression of EMT‐related markers (E‐cadherin, N‐cadherin, Claudin‐1, Vimentin, and Snail) was altered with FGFR4 blockade.
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| S8401 |
Erdafitinib (JNJ-42756493)Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂，具有潜在的抗肿瘤活性。 |
E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493 |
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| S7940 |
NSC12NSC12是一种可口服的FGF2/FGFR相互作用抑制剂，具有潜在的抗肿瘤的活性。 |
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| S8404 |
S49076S49076是一种新型的、有效的MET, AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。 |
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| S8503 |
BLU-554 (BLU554)BLU-554是一种有效的、高度选择性的、具有口服活性的FGFR4抑制剂，IC50为5 nM。对FGFR1-3的IC50范围为624-2203 nM。 |
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| S8578 |
PRN1371PRN1371是FGFR1-4的不可逆性共价抑制剂，对于FGFR1, 2, 3, 4和CSF1R的IC50分别为0.6、1.3、4.1、19.3、和8.1 nM。 |
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| S8493 |
PD-166866 (PD166866)PD-166866是一种合成类小分子，抑制FGFR1的酪氨酸激酶作用，对FGFR1具有高度选择性并抑制FGFR1的自我磷酸化活性。 |
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| S8548 |
Roblitinib (FGF401)FGF401是FGFR4选择性抑制剂，IC50为1.1 nM。它与FGFR4激酶区域可逆共价结合，对FGFR4的选择性至少是对检测的65种激酶的选择性的1000倍。 |
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| S7714 |
FIIN-2FIIN-2是一种不可逆的泛-FGFR抑制剂，对FGFR1/2/3/4的IC50分别为3.09 nM，4.3 nM，27 nM 和 45.3 nM。 |
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| S7665 |
CH5183284 (Debio-1347)CH5183284 是一种选择性口服有效的FGFR抑制剂，对FGFR1，FGFR2，FGFR3，和 FGFR4的IC50分别为 9.3 nM，7.6 nM，22 nM，和 290 nM 。Phase 1。 |
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| S7819 |
BLU9931BLU9931是一种有效的，选择性的，且不可逆的 FGFR4 抑制剂，IC50 为 3 nM，选择性比作用于 FGFR1/2/3分别高 297，184，和 50倍。 |
(E,G) Microscopic appearance of peritoneal dissemination of YTN16 (E) without BLU9931 and (G) with BLU9931 treatment for 3 weeks. (F,H) Microscopic features of s.c. tumor of YTN16 (F) without BLU9931 and (H) with BLU9931 treatment for 3 weeks. YTN16 tumor under treatment with BLU9931 does not form glandular structures.
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| S8192 |
SUN11602SUN11602是一种合成的小分子化合物，可模拟bFGF的神经保护活性、激活FGFR-1-MEK/ERK信号通路中关键信号分子。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1490 |
Ponatinib (AP24534)Ponatinib (AP24534)是一种新型有效的多靶点抑制剂，在无细胞试验中作用于Abl，PDGFRα，VEGFR2，FGFR1和Src，IC50分别为0.37 nM，1.1 nM，1.5 nM，2.2 nM和5.4 nM。 |
RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT.
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| S2183 |
BGJ398 (NVP-BGJ398|Infigratinib)BGJ398 (NVP-BGJ398)是一种有效的，选择性FGFR抑制剂，作用于FGFR1/2/3，在无细胞试验中IC50为0.9 nM/1.4 nM/1 nM，作用于FGFR比作用于FGFR4和VEGFR2选择性高40倍以上，对Abl， Fyn， Kit， Lck， Lyn和Yes几乎没有抑制活性。Phase 2。 |
Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIN3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 µM BGJ398, and 0.2 and 1 µM PD173074 were immunoblotted with the relevant antibodies. β-actin was used as a loading control. |
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| S1010 |
Nintedanib (BIBF 1120)Nintedanib (BIBF 1120) 尼达尼布是一种有效的三重血管激酶抑制剂，作用于VEGFR1/2/3， FGFR1/2/3和PDGFRα/β，在无细胞试验中IC50分别为34 nM/13 nM/13 nM， 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。 |
Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group |
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| S1264 |
PD173074PD173074是一种有效的FGFR1抑制剂，在无细胞试验中IC50约为25 nM，也能抑制VEGFR2，IC50为100-200 nM，作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。 |
FGFR inhibitors block signaling in FGFR2-fusion-expressing cells. Activation of FGFR2 and MAPK by FGFR2-AHCYL1 and its suppression by FGFR inhibitors. Lysates from NIH3T3 cells expressing FGFR2-AHCYL1 or EZR-ROS1 (control) treated with vehicle (DMSO), 0.2 and 1 uM BGJ398, and 0.2 and 1 uM PD173074 were immunoblotted with the relevant antibodies. β-Actin was used as a loading control.
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| S1018 |
Dovitinib (TKI-258, CHIR-258)Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂，在无细胞试验中对III型(FLT3/c-Kit)作用最强，IC50为1 nM/2 nM，同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs，IC50为8-13 nM，但对InsR，EGFR，c-Met，EphA2，Tie2，IGF-1R和HER2作用较弱。Phase 4。 |
Orthotopic xenografts of HNSCC cell lines (A) SCC-1 and (B) OSC-19 were treated with dovitinib (20 mg/kg/day). In addition, the OSC-19 xenografts were treated with +/ radiation therapy. Marker, mean for triplicate; bars, SE. Statistical significance by unpaired t-test, p < 0.05. |
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| S8754New |
Alofanib(RPT835)Alofanib(RPT835)是一种新型的、选择性FGFR2变构抑制剂，在KATO III细胞中对FGF2诱导的FRS2α磷酸化具有显著的抑制效果，IC50小于10 nM。在细胞中，它对依赖于FGF2的FGFR1和FGFR3磷酸化水平没有直接作用，对FGF2-FGFR2的结合没有影响。 |
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| s9031New |
Gambogenic acidGambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. |
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| S8609New |
Derazantinib(ARQ-087)Derazantinib(ARQ-087)是具有口服生物活性的FGFR抑制剂，对FGFR2、FGFR1、FGFR3的IC50分别为1.8 nM、4.5 nM和4.5 nM，对FGFR4的抑制活性较低，IC50为34 nM。它还能抑制RET、DDR2、PDGFRβ、VEGFR和KIT。 |
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| S5234New |
Nintedanib Ethanesulfonate SaltNintedanib is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. |
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| S2801 |
AZD4547AZD4547是一种新型选择性的FGFR抑制剂，靶向作用于FGFR1/2/3，在无细胞试验中IC50为0.2 nM/2.5 nM/1.8 nM，对FGFR4， VEGFR2(KDR)具有微弱的作用活性，对IGFR， CDK2和p38几乎没有作用活性。Phase 2/3。 |
FCM evaluating lung CD11b+/Gr1+ myeloid cells isolated from 4T1 tumor-bearing mice after 20 days of treatment with AZD4547 or control. Statistical significance was assessed by unpaired t test. |
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| S1107 |
Danusertib (PHA-739358)Danusertib (PHA-739358)是一种Aurora kinase抑制剂，作用于Aurora A/B/C，无细胞试验中IC50为13 nM/79 nM/61 nM，适度有效作用于Abl，TrkA，c-RET和FGFR1，对Lck，VEGFR2/3，c-Kit，CDK2等作用效果稍弱。Phase 2。 |
Mice bearing subcutaneous allografts of conditional patched mutant tumor cells were treated twice weekly with vehicle (saline) or 30 mg/kg PHA-739358. (B)Images of tumors. (C) Tumor weights. Each point represents a single tumor, and grey lines represent mean tumor weights, which were significantly different between vehicle and PHA-739358 treated mice (p < 0.05, based on paired two-tailed t-test).
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| S1084 |
Brivanib (BMS-540215)Brivanib (BMS-540215)是一种ATP竞争性的VEGFR2抑制剂，IC50为25 nM，对VEGFR-1和FGFR-1抑制作用适中，但比作用于PDGFR-β效果强240多倍。Phase 3。 |
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of Brivanib by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
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| S2769 |
Dovitinib (TKI-258) Dilactic AcidDovitinib (TKI-258) Dilactic Acid 是一种多靶点的RTK抑制剂，作用于III型(FLT3/c-Kit)最有效，IC50为1 nM/2 nM，也有效作用于IV型(FGFR1/3)和V型(VEGFR1-4)RTKs，IC50为8-13 nM，对InsR， EGFR， c-Met， EphA2， Tie2， IGFR1和HER2作用效果稍弱。Phase 4。 |
In vitro assays on CUX1-FGFR1-expressing Ba/F3 cells. a. IL-3 deprivation of Ba/F3 cells transduced with CUX1-FGFR1 resulted in transformation to growth factor independent growth. The mean growth ±SEM of three separate measurements over four consecutive days is presented. b. The dose-response curves of CUX1-FGFR1-transduced Ba/F3 cells, treated with TKI258 and PKC412 for 48 hours in the absence or presence of IL-3 (2 ng/ml) are presented. Points represent the average results of two experiments done in triplicate plotted with the curve-fitting GraphPad Prism 5 software; bars, SD. The calculated IC50 for each inhibitor is indicated. c. Western blot analyses of CUX1-FGFR1-transformed Ba/F3 cells after treatment with PKC412 and TKI258. Phosphorylation of CUX1-FGFR1 and its downstream effectors STAT5 and RPS6K decreased with increasing inhibitor concentrations. Expression of total CUX1-FGFR1, STAT5 and RPS6K remained unaffected. d. Effect of PKC412 and TKI258 on apoptosis of CUX1-FGFR1-expressing Ba/F3 cells after treatment for 48 hours. The percentage of apoptotic plus necrotic CUX1-FGFR1-transduced Ba/F3 cells is indicated.
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| S2774 |
MK-2461MK-2461是一种有效的，多靶点抑制剂，作用于c-Met(WT/mutants)，IC50为0.4-2.5 nM，对Ron，和Flt1作用效果稍弱；作用于c-Met比作用于FGFR1， FGFR2， FGFR3， PDGFRβ， KDR， Flt3， Flt4， TrkA和TrkB选择性高8到30倍。Phase 1/2。 |
Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
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| S1138 |
Brivanib Alaninate (BMS-582664)Brivanib Alaninate (BMS-582664)是BMS-540215的前体药物，是一种ATP竞争性的VEGFR2抑制剂，IC50为25 nM。 |
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| S7167 |
SSR128129ESSR128129E是口服效果较好的变构FGFR抑制剂，IC50为1.9μM，对别的关联RTKs无效果。 |
Western blot analysis of the expression and activation status (a) of pFGFR, pERK and Bim after treatment of API5-overexpressing cells (a) with either DMSO or SSR128129E.
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| S7057 |
LY2874455LY2874455是一个泛FGFR的抑制剂，对FGFR1，FGFR2, FGFR3, 和FGFR4的IC50值分别为2.8 nM, 2.6 nM, 6.4 nM,以及6 nM。并且也能抑制VEGFR2的活性，IC50为7 nM。Phase 1。 |
A: Overall structure of LY2874455/FGFR4 complex. B: The diagram of LY2874455. C: Fo-Fc omit map of LY2874455 in the FGFR4/LY2874455 complex. The electron density is superimposed with the final model. D: The DFG motif conformation of FGFR4. Active ApoFGFR4 DFG-in conformation is shown in blue (PDB: 4QQT); FGFR4/Ponatinib DFG-out conformation is shown in yellow (PDB: 4UXQ); FGFR4/BLU9931 DFG-in conformation is shown in pink (PDB: 4XCU); FGFR4/LY2874455 DFG-in conformation is shown in grey (this work). LY2874455 is highlighted in brown.
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| S7667 |
SU5402SU5402是一种有效的多靶点受体激酶抑制剂，对VEGFR2，FGFR1，和PDGF-Rβ的IC50分别为20 nM，30 nM，和510 nM。 |
Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.
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| S7765 |
Dovitinib (TKI258) LactateDovitinib (TKI258) Lactate是Dovitinib的乳酸盐，Dovitinib是一种多靶点的PTK抑制剂，主要对第III类(FLT3/c-Kit)发挥作用，IC50为1 nM/2 nM，对第IV 类(FGFR1/3)和第V 类(VEGFR1-4) RTKs也有效，IC50为8-13 nM，对InsR，EGFR，c-Met，EphA2，Tie2，IGFR1 和HER2作用较差。Phase 4。 |
(c) Percent survival for the AGS cancer cell line is shown with FGFR2 inhibitors of varying specificity. (d) The KatoIII diffuse gastric cancer cell line was treated with FGFR2 inhibitors of varying specificity. The Y-axis depicts percent survival versus the X-axis with log concentrations. In all panels, error bars represent standard error of the mean. The difference in percent cell survival between KatoIII and AGS cells was statistically significant (P <0.05) at the three highest concentrations of all drugs, except Brivanib which was only significant at the highest concentration. |
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| S8675 |
H3B-6527H3B-6527是一个高度选择性的共价FGFR4抑制剂，IC50 < 1.2 nM，其对FGFR4的选择性是对FGFR1-3选择性的250倍以上（对FGFR1-3的IC50s分别为320, 1290和1060 nM）。 |
KYSE150 and KYSE450 cells were treated each day with 1 μM H3B‐6527 or left untreated for three days, and lysates were immunoblotted with indicated antibodies. Western blotting demonstrated that the expression of EMT‐related markers (E‐cadherin, N‐cadherin, Claudin‐1, Vimentin, and Snail) was altered with FGFR4 blockade.
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| S8401 |
Erdafitinib (JNJ-42756493)Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂，具有潜在的抗肿瘤活性。 |
E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493 |
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| S7940 |
NSC12NSC12是一种可口服的FGF2/FGFR相互作用抑制剂，具有潜在的抗肿瘤的活性。 |
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| S8404 |
S49076S49076是一种新型的、有效的MET, AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。 |
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| S8503 |
BLU-554 (BLU554)BLU-554是一种有效的、高度选择性的、具有口服活性的FGFR4抑制剂，IC50为5 nM。对FGFR1-3的IC50范围为624-2203 nM。 |
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| S8578 |
PRN1371PRN1371是FGFR1-4的不可逆性共价抑制剂，对于FGFR1, 2, 3, 4和CSF1R的IC50分别为0.6、1.3、4.1、19.3、和8.1 nM。 |
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| S8493 |
PD-166866 (PD166866)PD-166866是一种合成类小分子，抑制FGFR1的酪氨酸激酶作用，对FGFR1具有高度选择性并抑制FGFR1的自我磷酸化活性。 |
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| S8548 |
Roblitinib (FGF401)FGF401是FGFR4选择性抑制剂，IC50为1.1 nM。它与FGFR4激酶区域可逆共价结合，对FGFR4的选择性至少是对检测的65种激酶的选择性的1000倍。 |
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| S7714 |
FIIN-2FIIN-2是一种不可逆的泛-FGFR抑制剂，对FGFR1/2/3/4的IC50分别为3.09 nM，4.3 nM，27 nM 和 45.3 nM。 |
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| S7665 |
CH5183284 (Debio-1347)CH5183284 是一种选择性口服有效的FGFR抑制剂，对FGFR1，FGFR2，FGFR3，和 FGFR4的IC50分别为 9.3 nM，7.6 nM，22 nM，和 290 nM 。Phase 1。 |
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| S7819 |
BLU9931BLU9931是一种有效的，选择性的，且不可逆的 FGFR4 抑制剂，IC50 为 3 nM，选择性比作用于 FGFR1/2/3分别高 297，184，和 50倍。 |
(E,G) Microscopic appearance of peritoneal dissemination of YTN16 (E) without BLU9931 and (G) with BLU9931 treatment for 3 weeks. (F,H) Microscopic features of s.c. tumor of YTN16 (F) without BLU9931 and (H) with BLU9931 treatment for 3 weeks. YTN16 tumor under treatment with BLU9931 does not form glandular structures.
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| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
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| S8192 |
SUN11602SUN11602是一种合成的小分子化合物，可模拟bFGF的神经保护活性、激活FGFR-1-MEK/ERK信号通路中关键信号分子。 |
