PF-04217903

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Cat No.

CEI-0061

Description

PF-04217903, with triazolopyrazine chemical structure, can potently inhibit c-Met with IC50 of 4.8 nM.

CAS_No

956905-27-4

Molecular Weight

372.38

Purity

>99%

Storage

2 years at -20 centigrade

Targets

c-Met

Molecular Formula

C19H16N8O

Chemical Name

2-(4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-1H-pyrazol-1-yl)ethanol

Solubility

DSMO 5 mg/mL Water

In vitro

PF-04217903, with triazolopyrazine chemical structure, can potently inhibit c-Met with IC50 of 4.8 nM. PF-04217903 is a high selective and ATP-competitive inhibitor, and PF-04217903 shows more than 1000-fold selective relative to 208 kinases. PF-04217903 shows inhibition to c-Met-driven processes such as cell growth (proliferation and survival), motility, invasion, and morphology in a variety of tumor cells.

In vivo

Complete inhibition of c-Met activity by PF-04217903 only led to partial tumor growth inhibition (38%-46%) in human xenograft models that express relatively high levels of c-Met. PF-04217903 can potently induce phospho-PDGFRbeta (platelet-derived growth factor receptor) levels in U87MG xenograft tumor.

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Project Description:

For research and industrial use only, not for personal medicinal use.

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