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FGFR Fibroblast Growth Factor Receptor

Inhibitors

Cat.No.  Name Information
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.
M1840 BGJ398 (Infigratinib) BGJ398 (Infigratinib) 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.
M10737 PRN1371 PRN1371 is a highly selective and potent inhibitor of FGFR1-4 and CSF1R against FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R IC50 The values are 0.6, 1.3, 4.1, 19.3, and 8.1 nM, respectively.
M10590 Alofanib (RPT835) Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells.
M10518 ASP5878 ASP5878 is a novel selective FGFR inhibitor with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3 and 4, respectively.
M10048 PF-05231023 PF-05231023 is an FGF21-receptor agonist, it is also a potential treatment for T2DM.
M10026 Futibatinib (TAS-120) Futibatinib (TAS-120) is an oral bioavailable, highly selective and irreversible FGFR inhibitor with IC50 of 3.9, 1.3, 1.6 and 8.3 nM against the four FGFR 1-4 subtypes, respectively. Futibatinib inhibited mutant and wild-type FGFR2 with IC50 similarity (wild-type FGFR2=0.9 nM; V5651 = 1 to 3 nM; N550H = 3.6 nM. E566G = 2.4 nM).
M9715 Erdafitinib Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan FGFR inhibitor with potential antineoplastic activity.
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.
M6158 ARQ-087 ARQ 087 is a novel, ATP competitive, small molecule, multi-kinase inhibitor with potent in vitro and in vivo activity against FGFR addicted cell lines and tumors. ARQ 087 exhibited IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3.
M6095 Roblitinib(FGF-401) FGF-401 is an inhibitor of FGFR4, with 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 Fisogatinib (BLU-554) Fisogatinib (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.
M3897 Ferulic Acid Ferulic Acid is a hydroxycinnamic acid and a type of organic compound found in the Ferula assafoetida L. or Ligusticum chuanxiong.



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