PF-04217903 Inhibitor CAS No. 956905-27-4

Cat. No.	Name	Size	Price
KI0017	PF-04217903	5 mg	$160
	PF-04217903	10 mg	$256
	PF-04217903	50 mg	$752
	PF-04217903	100 mg	$1392

Chemical Characteristic

Product Name	PF-04217903
CAS No.	956905-27-4
Molecular Weight	372.38
Formula	C₁₉H₁₆N₈O
Chemical Name	2-[4-[1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazol-1-yl]ethanol
Smiles	C(Cn1ncc(c1)c1nc2c(nc1)nnn2Cc1cc2cccnc2cc1)O
Chemical Structure

Biological activities

PF-04217903 is a novel ATP-competitive small-molecule inhibitor of c-Met kinase. PF-04217903 inhibits c-MET kinase with an extremely potent and exquisitely selective fashion. The IC50 of PF-04217903 are 5 nM against c-Met while its K_{i is 4 nM. ^[1] PF-04217903 shows more than 1,000-fold selectivity for c-Met compared with more than 150 kinases including VEGFR, PDGFR. PF-04217903 inhibits tumor cell proliferation, survival, migration/invasion in MET-amplified cell lines in vitro, and shows marked antitumor activity in tumor models harboring either MET gene amplification or a hepatocyte growth factor (HGF)/c-Met autocrine loop at well-tolerated dose levels in vivo. Antitumor efficacy of PF-04217903 is dose-dependent and reveals a strong correlation with inhibition of c-Met phosphorylation, downstream signaling, and tumor cell proliferation/survival.^[2] PF-04217903 at the dose of 30 and 10 mg/kg produces maximal inhibition of tumor growth in the c-MET amplified GTL-16 xenograft tumor model. PF-04217903 reveals low to moderate in vivo rat clearance, low volume distribution, and good oral bioavailability. PF-04217903 exhibits a better half-life and volume distribution profile. The pK^a and t^1/2 are 4.66 and 4.7 hours, respectively. ^[1] In human xenograft models that express relatively high levels of c-Met, complete inhibition of c-Met activity by PF-04217903 only leads to partial tumor growth inhibition (38%??6%) in vivo. The combination of PF-04217903 with Recepteur d'origine nantais (RON) short hairpin RNA (shRNA) knockdown in the HT29 model that also expresses activated RON kinase??nduced tumor cell apoptosis and results in enhanced antitumor efficacy (77%) compared with either PF-04217903 (38%) or RON shRNA alone (56%). PF-04217903 also reveals potent antiangiogenic properties in vivo. Furthermore, PF-04217903 strongly induces phospho-PDGFRβ (platelet-derived growth factor receptor) levels in U87MG xenograft tumors.^[2]}

Protocols

PF-04217903 is dissolved in 1% DMSO.^[1]

References

[1] 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, 55(18): 8091-8109. [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, 11(4): 1036-1047.

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