FIIN-1

Research use only, not for human use.

FIIN-1 (FGFR irreversible inhibitor-1) is an irreversible and selective FGFR inhibitor with Kd of 2.8, 6.9, 5.4, 120, 32 and 120 nM for FGFR1, FGFR2, FGFR3, FGFR4, Flt1, Flt14, respectively.

FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.

FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480 and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively. FIIN-1 (14 nM-46 μM; 72 hours) inhibits proliferation of FGF signaling-sensitive cancer cell lines.FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.Cell Proliferation Assay Cell Line:Stomach KATO III, SNU-16 and FU97 cells; Bladder RT4 cells; Kidney G-401 and G-402 cells; Lung SBC-3 and H520 cells; Pancreas A2.1 cells; Ovary A2780 and PA-1 cells; Bone RD-ES cellsConcentration:Incubation Time:72 hours Result:The EC50 of 70 nM for Bladder RT4 cell. The EC50 of 230 nM for Pancreas A2.1 cell. The EC50 of 2.3 μM for Bone RD-ES cell. EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively. EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively. EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively. EC50s of 0.014, 0.03 and 0.65 μM for Stomach KATO III, SNU-16, FU97 cells, respectively.Western Blot Analysis Cell Line:Serum-starved MCF10A cells that stably express iFGFR1 Concentration:20 nM Incubation Time:30 minutes Result:Blocked activation of iFGFR1 and phosphorylation of downstream effectors Erk1/2.

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Angiogenesis

FGFR

FGFR

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1256152-35-8

656.6

C32H39Cl2N7O4

>98% (HPLC)

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C(N1C=2C(CN(C1=O)C3=C(Cl)C(OC)=CC(OC)=C3Cl)=CN=C(NCCCCN(CC)CC)N2)C4=CC(NC(C=C)=O)=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years