PF-05274857 (hydrochloride) |
Catalog No.GC18599 |
PF-05274857 (clorhidrato) es un antagonista de Smo potente, selectivo, activo por vÍa oral y que penetra en el cerebro, con una IC50 de 5,8 nM y una Ki de 4,6 nM. PF-05274857 (clorhidrato) tiene potencial para la investigaciÓn de tipos de tumores, incluidos tumores cerebrales y metÁstasis cerebrales impulsadas por una vÍa Hh activada.
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Cas No.: 1613439-62-5
Sample solution is provided at 25 µL, 10mM.
Sonic hedgehog (Shh) signaling is initiated by binding of the ligand, Shh, to the receptor Patched 1, which relieves suppression by the associated receptor Smoothened (Smo). PF-05274857 is an antagonist which binds Smo (Ki = 4.6 nM), blocking Gli1 transcription in cells stimulated with Shh (IC50 = 2.7 nM). When administered orally, it distributes through plasma to skin and tumor and remains metabolically stable. PF-05274857 also penetrates the blood-brain barrier and inhibits Smo activity in the brain.
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