FIIN-3

Description

FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC₅₀s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively). 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 FGFR2^TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC₅₀s = 1.4-499 nM).

Uses

FIIN-?3 is FGFR inhibitor. It can be used in synthetic preparation and complex with EGFR kinase of crystal structure; development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.

Definition

ChEBI: N-[4-[[[(2,6-dichloro-3,5-dimethoxyanilino)-oxomethyl]-[6-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]amino]methyl]phenyl]-2-propenamide is a member of piperazines.