FGFR
信号通路图
研究领域
抑制剂选择性比较
FGFR产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1040 |
Sorafenib (BAY 43-9006) tosylateSorafenib (BAY 43-9006) tosylate是Raf-1和B-Raf的多重激酶抑制剂，无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT，对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib Tosylate 可诱导autophagy、apoptosis并激活ferroptosis，并具有抗肿瘤活性。 |
Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells. |
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| 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。Ponatinib (AP24534)可抑制自噬。 |
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 |
Infigratinib (BGJ398)Infigratinib (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, Intedanib, Vargatef, Ofev) 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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| S1035 |
Pazopanib HCl (GW786034 HCl)Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit和c-fms，在无细胞试验中IC50分别是10 nM，30 nM，47 nM，84 nM，74 nM，140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。 |
Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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| S7647New |
Lucitanib (E3810) hydrochlorideLucitanib (E-3810, AL3810) hydrochloride 是 Vascular endothelial growth factor receptor (VEGFR) 和 Fibroblast growth factor receptor (FGFR) 的双重抑制剂。 Lucitanib hydrochloride (E-3810, AL3810) 有效且选择性地抑制 VEGFR1、VEGFR2、VEGFR3、FGFR1 和 FGFR2，IC50值分别为7 nM、25 nM、10 nM、17.5 nM和82.5 nM。 |
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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。PD173074 可在胃癌细胞中抑制增殖并促进凋亡。 |
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)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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| S2801 |
AZD4547AZD4547 (ABSK 091)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。Danusertib 可诱导凋亡、细胞周期阻滞和自噬。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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| S1164 |
Lenvatinib (E7080)Lenvatinib (E7080)是一种多靶点抑制剂，无细胞试验中，作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效，IC50为4 nM/5.2 nM，对VEGFR1/Flt-1作用效果稍弱，作用于VEGFR2/3比作用于FGFR1， PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、Kit (c-Kit)和RET (c-RET)的抑制剂，并具有强效的抗肿瘤活性。Phase 3。 |
Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
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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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| S1181 |
ENMD-2076ENMD-2076 选择性地作用于 Aurora A 和 Flt3，IC50分别为14 nM和1.86 nM，作用于Aurora A比作用于Aurora B选择性高25倍，对RET、SRC、NTRK1/TRKA、CSF1R/FMS、VEGFR2/KDR、FGFR和PDGFRα作用效果稍弱。ENMD-2076 可抑制各种人类实体瘤和造血癌细胞系的生长，其IC50值为0.025至0.7μM，可诱导凋亡和G2/M期停滞。Phase 2。 |
Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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| S3012 |
PazopanibPazopanib (GW786034) 是一种新型多靶点的VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit 和 c-Fms/CSF1R抑制剂，无细胞试验中IC50分别为10 nM，30 nM，47 nM，84 nM，74 nM，140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。 |
Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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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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| S8024 |
Tyrphostin AG 1296Tyrphostin AG 1296 是一种PDGFR抑制剂，IC50为0.3-0.5 μM，对EGFR没有抑制活性。Tyrphostin AG1296 在抑制Swiss 3T3细胞中抑制 FGFR 和 c-Kit 的IC50值为12.3 μM和1.8 μM。Tyrphostin AG1296 可在A375R细胞中诱导剧烈的凋亡。 |
After inoculation with KAT4 cells, administration of compounds including MK-2206 (100 mg/kg), tyrphostin AG 1296 (100 mg/kg), or a combination of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) was performed. The combination of MK-2206 and tyrphostin AG 1296 induced significant apoptosis of KAT4 tumor cells in vivo measured by the terminal deoxynucleotidyl transferase dUTP nick end labeling assay (green), and nuclei were stained with Hoechst (blue). |
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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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| S8609 |
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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| 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, CHIR258) 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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| S5240 |
Lenvatinib (E7080) MesylateLenvatinib Mesylate (E7080)是一种合成、具有口服活性的 tyrosine kinase 的抑制剂，可抑制血管内皮生长因子受体(VEGFR1-3)，成纤维细胞生长因子受体(FGFR1-4)，血小板衍生生长因子受体(PDGFRα)，干细胞因子受体(Kit (c-Kit))，并在转染过程中重新排列(RET (c-RET))。甲磺酸来伐替尼具有潜在的抗肿瘤活性。 |
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| S8882 |
ODM-203ODM-203是FGFR 和 VEGFR的双重抑制剂，对重组FGFR1，FGFR2，FGFR3，FGFR4，VEGFR1，VEGFR2和VEGFR3的ic50分别为11 nM，16 nM，6 nM，35 nM，26 nM，9 nM，5 nM。 |
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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。Erdafitinib 也能结合RET (c-RET)、CSF-1R、PDGFR-α/PDGFR-β、FLT4、Kit (c-Kit)和VEGFR-2并可诱导细胞凋亡。 |
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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| S6539 |
ASP5878ASP5878是新型的FGFR选择性抑制剂，对重组FGFR1、FGFR2、FGFR3和FGFR4的IC50分别为0.47, 0.60, 0.74和3.5 nM。 |
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| S8754 |
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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| S7940 |
NSC12NSC12 (NSC 172285)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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| S6526 |
SKLB 610SKLB-610是一种多靶点的酪氨酸激酶 (tyrosine kinases)抑制剂。它对VEGFR2的抑制作用最为有效，是FGFR2和PDGFR的弱抑制剂。 |
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| S8404 |
S49076S49076是一种新型的、有效的Met (c-Met), AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。 |
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| S0088 |
Pemigatinib (INCB054828)Pemigatinib (INCB054828, Pemazyre)是一种口服活性的 FGFR 的选择性抑制剂，对于FGFR1、FGFR2、FGFR3和FGFR4的IC50分别为0.4 nM、0.5 nM、1.2 nM和30 nM。Pemigatinib（INCB054828）具有治疗胆管癌的潜力。 |
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| S2300 |
Ferulic AcidFerulic Acid (Fumalic) 是一种羟基肉桂酸，是在Ferula assafoetida L或Ligusticum chuanxiong中发现的一种有机化合物。Ferulic acid 是一种新型的 fibroblast growth factor receptor (FGFR) 抑制剂，对FGFR1和FGFR2的IC50分别为3.78 μM和12.5 μM。 |
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| S9031 |
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. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination. |
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| S8503 |
Fisogatinib (BLU-554)Fisogatinib (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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| S8161 |
ON123300ON123300是有效的多靶点激酶抑制剂，对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。 |
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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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| S8965 |
BO-264BO-264 是一种有效的 transforming acidic coiled-coil 3 (TACC3) 的口服抑制剂，IC50值为188 nM，Kd值为1.5 nM。BO-264 可特异性地阻断 FGFR3-TACC3 融合蛋白的功能。BO-264 可诱导SAC依赖的有丝分裂阻滞、凋亡和具有抗肿瘤活性的DNA损伤。 |
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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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| S8848 |
Futibatinib (TAS-120)Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
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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 |
Zoligratinib (Debio-1347)Zoligratinib (Debio-1347, CH5183284, FF284)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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| S5234 |
Nintedanib Ethanesulfonate SaltNintedanib (Intedanib, BIBF 1120) 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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| 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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| S0487 |
SulfatinibSulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib)是一种有效的、具有高度选择性的 tyrosine kinase 的抑制剂，对于 VEGFR1、VEGFR2、VEGFR3、FGFR1 和 CSF1R 的IC50值分别为2 nM、24 nM、1 nM、15 nM和4 nM。Sulfatinib 在针对晚期NET患者的实验中显示出令人鼓舞的抗肿瘤活性和可控毒性。 |
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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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1040 |
Sorafenib (BAY 43-9006) tosylateSorafenib (BAY 43-9006) tosylate是Raf-1和B-Raf的多重激酶抑制剂，无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT，对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib Tosylate 可诱导autophagy、apoptosis并激活ferroptosis，并具有抗肿瘤活性。 |
Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells. |
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| 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。Ponatinib (AP24534)可抑制自噬。 |
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 |
Infigratinib (BGJ398)Infigratinib (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, Intedanib, Vargatef, Ofev) 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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| S1035 |
Pazopanib HCl (GW786034 HCl)Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit和c-fms，在无细胞试验中IC50分别是10 nM，30 nM，47 nM，84 nM，74 nM，140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。 |
Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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| S7647New |
Lucitanib (E3810) hydrochlorideLucitanib (E-3810, AL3810) hydrochloride 是 Vascular endothelial growth factor receptor (VEGFR) 和 Fibroblast growth factor receptor (FGFR) 的双重抑制剂。 Lucitanib hydrochloride (E-3810, AL3810) 有效且选择性地抑制 VEGFR1、VEGFR2、VEGFR3、FGFR1 和 FGFR2，IC50值分别为7 nM、25 nM、10 nM、17.5 nM和82.5 nM。 |
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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。PD173074 可在胃癌细胞中抑制增殖并促进凋亡。 |
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)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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| S2801 |
AZD4547AZD4547 (ABSK 091)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。Danusertib 可诱导凋亡、细胞周期阻滞和自噬。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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| S1164 |
Lenvatinib (E7080)Lenvatinib (E7080)是一种多靶点抑制剂，无细胞试验中，作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效，IC50为4 nM/5.2 nM，对VEGFR1/Flt-1作用效果稍弱，作用于VEGFR2/3比作用于FGFR1， PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、Kit (c-Kit)和RET (c-RET)的抑制剂，并具有强效的抗肿瘤活性。Phase 3。 |
Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
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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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| S1181 |
ENMD-2076ENMD-2076 选择性地作用于 Aurora A 和 Flt3，IC50分别为14 nM和1.86 nM，作用于Aurora A比作用于Aurora B选择性高25倍，对RET、SRC、NTRK1/TRKA、CSF1R/FMS、VEGFR2/KDR、FGFR和PDGFRα作用效果稍弱。ENMD-2076 可抑制各种人类实体瘤和造血癌细胞系的生长，其IC50值为0.025至0.7μM，可诱导凋亡和G2/M期停滞。Phase 2。 |
Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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| S3012 |
PazopanibPazopanib (GW786034) 是一种新型多靶点的VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit 和 c-Fms/CSF1R抑制剂，无细胞试验中IC50分别为10 nM，30 nM，47 nM，84 nM，74 nM，140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。 |
Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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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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| S8024 |
Tyrphostin AG 1296Tyrphostin AG 1296 是一种PDGFR抑制剂，IC50为0.3-0.5 μM，对EGFR没有抑制活性。Tyrphostin AG1296 在抑制Swiss 3T3细胞中抑制 FGFR 和 c-Kit 的IC50值为12.3 μM和1.8 μM。Tyrphostin AG1296 可在A375R细胞中诱导剧烈的凋亡。 |
After inoculation with KAT4 cells, administration of compounds including MK-2206 (100 mg/kg), tyrphostin AG 1296 (100 mg/kg), or a combination of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) was performed. The combination of MK-2206 and tyrphostin AG 1296 induced significant apoptosis of KAT4 tumor cells in vivo measured by the terminal deoxynucleotidyl transferase dUTP nick end labeling assay (green), and nuclei were stained with Hoechst (blue). |
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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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| S8609 |
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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| 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, CHIR258) 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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| S5240 |
Lenvatinib (E7080) MesylateLenvatinib Mesylate (E7080)是一种合成、具有口服活性的 tyrosine kinase 的抑制剂，可抑制血管内皮生长因子受体(VEGFR1-3)，成纤维细胞生长因子受体(FGFR1-4)，血小板衍生生长因子受体(PDGFRα)，干细胞因子受体(Kit (c-Kit))，并在转染过程中重新排列(RET (c-RET))。甲磺酸来伐替尼具有潜在的抗肿瘤活性。 |
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| S8882 |
ODM-203ODM-203是FGFR 和 VEGFR的双重抑制剂，对重组FGFR1，FGFR2，FGFR3，FGFR4，VEGFR1，VEGFR2和VEGFR3的ic50分别为11 nM，16 nM，6 nM，35 nM，26 nM，9 nM，5 nM。 |
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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。Erdafitinib 也能结合RET (c-RET)、CSF-1R、PDGFR-α/PDGFR-β、FLT4、Kit (c-Kit)和VEGFR-2并可诱导细胞凋亡。 |
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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| S6539 |
ASP5878ASP5878是新型的FGFR选择性抑制剂，对重组FGFR1、FGFR2、FGFR3和FGFR4的IC50分别为0.47, 0.60, 0.74和3.5 nM。 |
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| S8754 |
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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| S7940 |
NSC12NSC12 (NSC 172285)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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| S6526 |
SKLB 610SKLB-610是一种多靶点的酪氨酸激酶 (tyrosine kinases)抑制剂。它对VEGFR2的抑制作用最为有效，是FGFR2和PDGFR的弱抑制剂。 |
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| S8404 |
S49076S49076是一种新型的、有效的Met (c-Met), AXL/MER和FGFR1/2/3抑制剂，IC50低于20 nM。 |
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| S0088 |
Pemigatinib (INCB054828)Pemigatinib (INCB054828, Pemazyre)是一种口服活性的 FGFR 的选择性抑制剂，对于FGFR1、FGFR2、FGFR3和FGFR4的IC50分别为0.4 nM、0.5 nM、1.2 nM和30 nM。Pemigatinib（INCB054828）具有治疗胆管癌的潜力。 |
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| S2300 |
Ferulic AcidFerulic Acid (Fumalic) 是一种羟基肉桂酸，是在Ferula assafoetida L或Ligusticum chuanxiong中发现的一种有机化合物。Ferulic acid 是一种新型的 fibroblast growth factor receptor (FGFR) 抑制剂，对FGFR1和FGFR2的IC50分别为3.78 μM和12.5 μM。 |
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| S9031 |
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. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination. |
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| S8503 |
Fisogatinib (BLU-554)Fisogatinib (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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| S8161 |
ON123300ON123300是有效的多靶点激酶抑制剂，对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。 |
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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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| S8965 |
BO-264BO-264 是一种有效的 transforming acidic coiled-coil 3 (TACC3) 的口服抑制剂，IC50值为188 nM，Kd值为1.5 nM。BO-264 可特异性地阻断 FGFR3-TACC3 融合蛋白的功能。BO-264 可诱导SAC依赖的有丝分裂阻滞、凋亡和具有抗肿瘤活性的DNA损伤。 |
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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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| S8848 |
Futibatinib (TAS-120)Futibatinib (TAS-120) is an irreversible fibroblast growth factor receptor (FGFR) inhibitor which inhibits all 4 subtypes of FGFR with enzyme IC50 values of 1.8 nM, 1.4 nM, 1.6 nM and 3.7 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
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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 |
Zoligratinib (Debio-1347)Zoligratinib (Debio-1347, CH5183284, FF284)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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| S5234 |
Nintedanib Ethanesulfonate SaltNintedanib (Intedanib, BIBF 1120) 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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| 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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| S0487 |
SulfatinibSulfatinib (HMPL-012, Sufatinib, Surfatinib, Surufatinib)是一种有效的、具有高度选择性的 tyrosine kinase 的抑制剂，对于 VEGFR1、VEGFR2、VEGFR3、FGFR1 和 CSF1R 的IC50值分别为2 nM、24 nM、1 nM、15 nM和4 nM。Sulfatinib 在针对晚期NET患者的实验中显示出令人鼓舞的抗肿瘤活性和可控毒性。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| 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。 |
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