An ATP-competitive

PF-562271 (besylate) – 1 mg

Brand:
Cayman
CAS:
939791-38-5
Storage:
-20
UN-No:
Non-Hazardous - /

Focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) are non-receptor tyrosine kinases that constitute the FAK subfamily and play a vital role in many oncogenic pathways.{15630} PF-562271 is an ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) that demonstrates 10-fold reduced potency for PYK2 (IC50 = 14 nM) and >100-fold selectivity against other protein kinases.{29911} PF-562271 inhibits FAK phosphorylation with an EC50 value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.{29911,29912}  

 

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Description

An ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) and PYK2 (IC50 = 14 nM); inhibits FAK phosphorylation (EC50 = 93 ng/ml) in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models

Formal name: N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-methanesulfonamide, monobenzenesulfonate

Synonyms: 

Molecular weight: 665.7

CAS: 939791-38-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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