FGFR4-IN-8 (Compound 7v) is an ATP-competitive inhibitor that covalently and highly selectively targets both the wild-type and gatekeeper mutant forms of FGFR4. It shows excellent inhibitory potency with IC50s of 0.5 nM for FGFR4, 0.25 nM for FGFR4 V550L, 1.6 nM for FGFR4 V550M, and 931 nM for FGFR4 C552S. Additionally, FGFR4-IN-8 has a potent antiproliferative effect on Hep3B hepatocellular carcinoma cells, with an IC50 of 29 nM, and demonstrates moderate antitumor efficacy in vivo in a Huh-7 xenograft model in nude mice [1].

FGFR2-IN-1 is an FGFR inhibitor that inhibits FGFR1, FGFR2, and FGFR3 with IC50s of 460, 140, and 2200 nM, respectively.FGFR2-IN-1 can be used for the study of cancers associated with FGFR2.CAS 번호13460-73-81-1

ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).

S49076 HCl (S-49076 Hydrochloride) is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 HCl potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 HCl inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 HCl was established and correlated well with impact on tumor growth.