PF-05274857 (hydrochloride) |
| Catalog No.GC18599 |
PF-05274857 (hydrochloride) is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-05274857 (hydrochloride) has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
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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