FGFR-IN-8

Names

[ CAS No. ]:
2640217-64-5

[ Name ]:
FGFR-IN-8

Biological Activity

[Description]:

FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR

[Target]

FGFR1:<0.5 nM (IC50)

V564F-FGFR2:189.1 nM (IC50)

N549H-FGFR2:<0.5 nM (IC50)

V555M-FGFR3:22.6 nM (IC50)

FGFR3:<0.5 nM (IC50)

FGFR4:7.30 nM (IC50)

V561M-FGFR1:262.5 nM (IC50)

K650E-FGFR3:<0.5 nM (IC50)

K650M-FGFR3:4.8 nM (IC50)


[References]

[1]. Ryu S, et al. Identification of Pyridinyltriazine Derivatives as Potent panFGFR Inhibitors against Gatekeeper Mutants for Overcoming Drug Resistance. J Med Chem. 2022 Apr 28;65(8):6017-6038.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H31Cl2N9O2

[ Molecular Weight ]:
584.50

Related Compounds