FIIN-2

Modify Date: 2025-08-21 14:05:12

FIIN-2 Structure
FIIN-2 structure
Common Name FIIN-2
CAS Number 1633044-56-0 Molecular Weight 634.727
Density 1.3±0.1 g/cm3 Boiling Point N/A
Molecular Formula C35H38N8O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of FIIN-2


FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

 Names

Name fiin-2
Synonym More Synonyms

 FIIN-2 Biological Activity

Description FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
Related Catalog
Target

FGFR1:3.1 nM (IC50)

FGFR2:4.3 nM (IC50)

FGFR3:27 nM (IC50)

FGFR4:45 nM (IC50)

In Vitro FIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F[1].
In Vivo Treatment of fish in the embryonic state with either FIIN-2 causes defects to the posterior mesoderm similar to the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFR inhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryonic zebrafish[1].
Cell Assay TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of the compounds. After 72 h the cells are assessed by MTS tetrazolium assay[1].
References

[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):E4869-4877.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Molecular Formula C35H38N8O4
Molecular Weight 634.727
Exact Mass 634.301575
PSA 115.40000
LogP 1.82
Index of Refraction 1.666
Storage condition -20℃

 Synonyms

N-(4-((3-(3,5-dimethoxyphenyl)-7-((4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide
FIIN2
2-Propenamide, N-[4-[[3-(3,5-dimethoxyphenyl)-3,4-dihydro-7-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-oxopyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl]phenyl]-
N-(4-{[3-(3,5-Dimethoxyphenyl)-7-{[4-(4-methyl-1-piperazinyl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)acrylamide
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