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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M9596 | Pemigatinib | Pemigatinib (INCB054828) is an orally bioavailable inhibitor of FGFR with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. |
| M9532 | BO-264 | BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. |
| M9296 | 2,5-Dihydroxybenzoic acid | 2,5-Dihydroxybenzoic acid is a derivative of benzoic, it is also an inhibitor of fibroblast growth factors. |
| M8938 | FIIN-3 | FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor with IC50 values of 13.1, 21, 31.4 and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
| M8936 | FGFR4-IN-1 | FGFR4-IN-1 is a potent and selective FGFR4 inhibitor with IC50 of 0.7 nM. |
| M6095 | FGF-401 | FGF-401 is an inhibitor of FGFR4 extracted from patent WO2015059668A1, compound example 83; has an IC50 of 1.9 nM. |
| M5274 | PD-166866 (PD166866) | PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1. |
| M5253 | BLU-9931 | BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively. |
| M5242 | H3B-6527 | H3B-6527 (H3 Biomedicine) is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice. |
| M5237 | BLU-554 | BLU-554 is a potent, highly-selective, oral FGFR4 inhibitor with an IC50 value of 5 nM. The IC50s for FGFR1-3 is 624-2203 nM. |
| M5235 | NSC12 | NSC12 is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity. |
| M4977 | AZ5104 | AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. |
| M3698 | SKLB610 | SKLB610 is a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. |
| M3617 | LY2874455 | LY2874455 is a novel and potent FGF/FGFR inhibitor. |
| M3031 | SSR128129E | SSR128129E is an orally-active and allosteric FGFR1 inhibitor with IC50 of 1.9 μM, while not affecting other related RTKs. |
| M1875 | PD173074 | PD173074 is a selective FGFR1 and FGFR3 inhibitor with IC50 values of 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. |
| M1840 | BGJ398 | BGJ398 is a potent and selective FGFR kinase inhibitor with IC50 values of 0.9 nM, 1.4 nM, 1 nM and 60 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
| M1721 | AZD4547 | AZD4547 is a potent, selective and orally active pan-FGFR inhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively. |
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