PF-04217903 (mesylate)

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

Product Specifications

CAS Number

[956906-93-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, 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-mesylate.html

Purity

99.82

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C20H20N8O4S

Molecular Weight

468.49

Precautions

H302, H315, H319, 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]Shojaei F, et al. HGF/c-Met acts as an alternative angiogenic pathway in sunitinib-resistant tumors. Cancer Res, 2010, 70 (24), 10090-10100.|[3]Krumbach R, et al. Primary resistance to cetuximab in a panel of patient-derived tumour xenograft models: activation of MET as one mechanism for drug resistance. Eur J Cancer, 2011, 47 (8), 1231-1243.