FIIN-2 Chemical Properties

Density 

1.306±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥31.75 mg/mL in DMSO; insoluble in H2O; ≥3.39 mg/mL in EtOH with gentle warming

form 

solid

pka

13.51±0.70(Predicted)

color 

White to off-white

FIIN-2 Usage And Synthesis

Description

FIIN-2 is an irreversible FGFR inhibitor with IC₅₀ values of 3.09, 4.3, 27, and 45.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. It has been shown to inhibit cell proliferation of transformed Ba/F3 cell lines and demonstrates antiproliferative activity in cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2. By inhibiting FGFR in a zebrafish developmental model, FIIN-2 caused mild to severe alterations in tail morphogenesis similar to the phenotypes reported following genetic knockdown of FGFR.

Uses

FIIN 2 is FGFR inhibitor. It can be used in biological study of DFG-out mode of inhibition by an irreversible Type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors

in vivo

IC 50

FGFR1: 3.1 nM (IC₅₀); FGFR2: 4.3 nM (IC₅₀); FGFR3: 27 nM (IC₅₀); FGFR4: 45 nM (IC₅₀)

References

[1] LI TAN. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014, 111 45: E4869-77. DOI: 10.1073/pnas.1403438111