An inhibitor of FGFRs
FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC50s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively).1 It is selective for FGFRs over a panel of 456 kinases at a concentration of 1 μM, however, it does inhibit EGFR (IC50 = 204 nM). FIIN-3 inhibits growth of Ba/F3 cells that are dependent on the kinase activity of wild-type FGFR1-4 as well as gatekeeper mutant FGFR2 and FGFR3 (EC50s = <1-69 nM) and inhibits FGFR-dependent signaling in a concentration-dependent manner in FGFR2TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC50s = 1.4-499 nM).
1.Tan, L., Wang, J., Tanizaki, J., et al.Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitorsProc. Natl. Acad. Sci. USA111(45)E4869-E4877(2014)
Cell experiment: | TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of FIIN-3. After 72 h the cells are assessed by MTS tetrazolium assay[1]. |
参考文献: [1]. Tan L et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A, 2014 Nov 11, 111(45):E4869-77 | |
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