PF 5274857 hydrochloride

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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% (HPLC)
Literature (1)

Biological Activity for PF 5274857 hydrochloride

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 5274857 hydrochloride

PF 5274857 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for PF 5274857 hydrochloride

M. Wt 473.42
Formula C20H25ClN4O3S.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1613439-62-5
PubChem ID 90489027
Smiles CC1=CN=C(C2=CC(N3CCN(C(CCS(C)(=O)=O)=O)CC3)=NC=C2Cl)C(C)=C1.Cl

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.

Solubility Data for PF 5274857 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 47.34 100
DMSO 47.34 100

Preparing Stock Solutions for PF 5274857 hydrochloride

The following data is based on the product molecular weight 473.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.11 mL 10.56 mL 21.12 mL
5 mM 0.42 mL 2.11 mL 4.22 mL
10 mM 0.21 mL 1.06 mL 2.11 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets for PF 5274857 hydrochloride

References for PF 5274857 hydrochloride

References are publications that support the biological activity of the product.

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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Citations for PF 5274857 hydrochloride

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