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PF-04217903 methanesulfonate

Catalog No. T12417 CAS 956906-93-7

PF-04217903 methanesulfonate is a potent ATP-competitive inhibitor of c-Met kinase (Ki of 4.8 nM for human c-Met).

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PF-04217903 methanesulfonate, CAS 956906-93-7

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	PF-04217903 methanesulfonate is a potent ATP-competitive inhibitor of c-Met kinase (Ki of 4.8 nM for human c-Met).
Targets&IC50	human c-Met(ki):ki:4.8 nM
In vitro	PF-04217903 induces apoptosis of GTL-16 cells (IC50=31 nM) [1]. PF-04217903 methanesulfonate also inhibits HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines such as human NCI-H441 lung carcinoma and HT29 colon carcinoma with IC50 values comparable with those for inhibition of c-Met phosphorylation in these cell lines (IC50= 7-12.5 nM)[1].
In vivo	PF-04217903 methanesulfonate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 methanesulfonate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors[1].

Molecular Weight	468.49
Formula	C20H20N8O4S
CAS No.	956906-93-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (106.73 mM), Need ultrasonic

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

References and Literature

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.

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Keywords

PF-04217903 methanesulfonate 956906-93-7 蛋白酪氨酸激酶 c-Met/HGFR PF04217903 methanesulfonate PF 04217903 methanesulfonate Inhibitor inhibitor inhibit

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