PF-05274857 (hydrochloride) |
| Catalog No.GC18599 |
PF-05274857(염산염)은 IC50이 5.8nM이고 Ki가 4.6nM인 Smo의 강력하고 선택적인 경구 활성 및 뇌 침투 길항제입니다. PF-05274857(염산염)은 활성화된 Hh 경로에 의해 유도되는 뇌종양 및 뇌 전이를 포함한 종양 유형 연구에 대한 잠재력이 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1613439-62-5
Sample solution is provided at 25 µL, 10mM.
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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.
Review for PF-05274857 (hydrochloride)
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
Review for PF-05274857 (hydrochloride)
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