FGFR-IN-8

Modify Date: 2024-04-06 16:31:17

FGFR-IN-8 Structure
FGFR-IN-8 structure
Common Name FGFR-IN-8
CAS Number 2640217-64-5 Molecular Weight 584.50
Density N/A Boiling Point N/A
Molecular Formula C27H31Cl2N9O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of FGFR-IN-8


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].

 Names

Name FGFR-IN-8

 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
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