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FIIN-1

Catalog No. T37426 CAS 1256152-35-8

Potent, irreversible FGFR inhibitor (Kd values are 2.8, 5.4, 6.9 and 120 nM for FGFR1, FGFR3, FGFR2 and FGFR4 respectively); acts at the ATP binding site. Also irreversibly inhibits FLT-1, FLT-4 and VEGFR-2 (Kd values are 32, 120 and 210 nM respectively); displays limited activity (Kd >500 nM) at other kinases. Exhibits antiproliferative activity in FGFR3- and FGFR1-transformed Ba/F3 cells (EC50 values are 10 and 14 nM respectively). Derived from the reversible FGFR inhibitor, PD 173074.

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FIIN-1, CAS 1256152-35-8

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

Potent, irreversible FGFR inhibitor (Kd values are 2.8, 5.4, 6.9 and 120 nM for FGFR1, FGFR3, FGFR2 and FGFR4 respectively); acts at the ATP binding site. Also irreversibly inhibits Flt-1, Flt-4 and VEGFR-2 (Kd values are 32, 120 and 210 nM respectively); displays limited activity (Kd >500 nM) at other kinases. Exhibits antiproliferative activity in FGFR3- and FGFR1-transformed Ba/F3 cells (EC50 values are 10 and 14 nM respectively). Derived from the reversible FGFR inhibitor, PD 173074.

Targets&IC50

FGFR4:189 nM (IC50), FGFR3:5.4 nM (Kd), FGFR1:9.2 nM (IC50), FGFR2:6.9 nM (Kd), FGFR4:120 nM (Kd), FGFR3:11.9 nM (IC50), FGFR1:2.8 nM (Kd), FGFR2:6.2 nM (IC50)

Molecular Weight	656.61
Formula	C32H39Cl2N7O4
CAS No.	1256152-35-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: Soluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Zhou (2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem.Biol. 17 285 PMID:20338520

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

FIIN-1 1256152-35-8 FIIN 1 FIIN1 Inhibitor inhibitor inhibit

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