PF 5274857 hydrochloride

Key Product Details

Product Description

PF 5274857 hydrochloride is a high affinity and selective Smoothened (Smo) receptor antagonist (K_i = 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.

Product Specifications for PF 5274857 hydrochloride

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

• Rohner 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. 2011 PMID: 22084163

Product Documents for PF 5274857 hydrochloride