PF 5274857 hydrochloride

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5262/10
5262/50
PF 5274857 hydrochloride | CAS No. 1613439-62-5 | Smoothened Receptor Antagonists
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Description: High affinity and selective Smoothened (Smo) receptor antagonist

Chemical Name: 1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride

Purity: ≥98%

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Biological Activity

PF 5274857 hydrochloride is a high affinity and selective Smoothened (Smo) receptor antagonist (Ki = 4.6 nM). Exhibits >1000-fold selectivity for Smo over a panel of other receptors, ion channels and enzymes. Inhibits Shh-induced Hedgehog signaling in MEF cells. Induces tumor regression in a medulloblastoma allograft mouse model. Orally available and brain penetrant.

Technical Data

M.Wt:
473.42
Formula:
C20H25ClN4O3S.HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at RT
CAS No:
1613439-62-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

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