PF 5274857 hydrochloride

Cat. No. 5262

PF 5274857 hydrochloride C20H25ClN4O3S.HCl [1613439-62-5]

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

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Rohner et al (2011) Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Mol.Cancer Ther. 11 57. PMID: 22084163.

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