PF-04217903

PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties[1][2].

Product Specifications

CAS Number

[956905-27-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H320, H335

Target

C-Met/HGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PF-04217903.html

Purity

99.85

Solubility

DMSO : 20 mg/mL (ultrasonic) |Ethanol : < 1 mg/mL (ultrasonic)

Smiles

OCCN1N=CC(C2=NC3=C(N=C2)N=NN3CC4=CC5=CC=CN=C5C=C4)=C1

Molecular Formula

C19H16N8O

Molecular Weight

372.38

Precautions

H302, H315, H320, H335

References & Citations

[1]Timofeevski SL, et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry, 2009, 48 (23), 5339-5349.|[2]Zou HY, et al. Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor. Mol Cancer Ther. 2012 Apr;11 (4) :1036-47.|[3]Cui JJ, et al. Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2- (4- (1- (quinolin-6-ylmethyl) -1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl) -1H-pyrazol-1-yl) ethanol (PF-04217903) for the treatment of cancer. J Med Chem. 2012 Sep 27;55 (18) :8091-109.