PF-05274857 (hydrochloride) |
| カタログ番号GC18599 |
PF-05274857 (塩酸塩) は、5.8 nM の IC50 と 4.6 nM の Ki を持つ、Smo の強力で選択的な経口活性の脳浸透性アンタゴニストです。 PF-05274857 (塩酸塩) は、活性化された Hh 経路によって駆動される脳腫瘍および脳転移を含む腫瘍タイプの研究の可能性を秘めています。
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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