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FIIN-1

Catalog No. T37426   CAS 1256152-35-8
Synonyms: FGFR irreversible inhibitor-1

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 inhibited FGFR1, FGFR2, FGFR3, FGFR4, with IC50 of 9.2, 6.2, 11.9 and 189 nM. FIIN-1 inhibited FGFR1, FGFR2, FGFR3 and FGFR4, with IC50s of 9.2, 6.2, 11.9 and 189 nM, respectively.

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FIIN-1 Chemical Structure
FIIN-1, CAS 1256152-35-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 72.00
2 mg In stock $ 105.00
5 mg In stock $ 213.00
10 mg In stock $ 347.00
25 mg In stock $ 578.00
50 mg In stock $ 825.00
100 mg In stock $ 1,090.00
500 mg In stock $ 2,230.00
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Purity: 97.30%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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 inhibited FGFR1, FGFR2, FGFR3, FGFR4, with IC50 of 9.2, 6.2, 11.9 and 189 nM. FIIN-1 inhibited FGFR1, FGFR2, FGFR3 and FGFR4, with IC50s of 9.2, 6.2, 11.9 and 189 nM, respectively.
Targets&IC50 FGFR4:120 nM (Kd), FGFR4:189 nM (IC50), FGFR3:11.9 nM (IC50), FGFR3:5.4 nM (Kd), FGFR1:2.8 nM (Kd), FGFR1:9.2 nM (IC50), FGFR2:6.2 nM (IC50), FGFR2:6.9 nM (Kd)
In vitro FIIN-1 (14 nM-46 μM; 72 h; ) inhibits the proliferation of FGF signaling-sensitive cancer cell lines. The EC50s of 70 nM, 230 nM, 2.3 μM, for Bladder RT4, Pancreas A2.1, Bone RD-ES cells. 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, and FU97 cells, respectively.[1]
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.[1]
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.[1]
Synonyms FGFR irreversible inhibitor-1
Molecular Weight 656.6
Formula C32H39Cl2N7O4
CAS No. 1256152-35-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (68.53 mM)

TargetMolReferences and Literature

1. Zhou W, et al. A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol. 2010 Mar 26;17(3):285-95.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Membrane Protein-targeted Compound Library Inhibitor Library Kinase Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Lung Cancer Compound Library Covalent Inhibitor Library

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Keywords

FIIN-1 1256152-35-8 Angiogenesis Tyrosine Kinase/Adaptors FGFR FIIN 1 FGFR irreversible inhibitor-1 FIIN1 inhibitor inhibit

 

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