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PF 5274857 hydrochloride
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.
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PF 5274857 hydrochloride
Technical Data for PF 5274857 hydrochloride
|Storage||Desiccate at RT|
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|
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.
|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|
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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