2014年8月4日星期一

PF-04449913 inhibitors

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor.
IC50 value: 5 nM [1]
Target: smoothened
PF-04449913, a Smoothened inhibitor was identified possessing excellent potency and physical properties that translate to an attractive predicted human pharmacokinetic profile. PF-04449913 was advanced to in vivo tumor growth inhibition studies, preclinical safety studies, and ultimately to human clinical trials. These results will be reported in separate disclosures.
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