A selective class I c-Met kinase inhibitor (Ki = 4.8 nM) that inhibits tumor cell proliferation

PF-04217903 – 5 mg

Brand:
Cayman
CAS:
956905-27-4
Storage:
-20
UN-No:
Non-Hazardous - /

MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}  

 

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Description

A selective class I c-Met kinase inhibitor (Ki = 4.8 nM) that inhibits tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM); shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop

Formal name: 4-[1-(6-quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol

Synonyms: 

Molecular weight: 372.4

CAS: 956905-27-4

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 Death||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling

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