PF 5274857 hydrochloride
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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 473.42. Batch specific molecular weights may vary from batch to batch due to solvent 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|
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
If you know of a relevant reference for PF 5274857 hydrochloride, please let us know.
View Related Products by Product Action
Keywords: PF 5274857 hydrochloride, PF 5274857 hydrochloride supplier, PF5274857, hydrochloride, high, affinity, selective, smoothened, Smo, receptor, antagonist, hedgehog, signaling, antitumor, brain, penetrant, orally, available, active, Smoothened, Receptors, Hedgehog, Signaling, 5262, Tocris Bioscience
Citations for PF 5274857 hydrochloride
Citations are publications that use Tocris products.
Currently there are no citations for PF 5274857 hydrochloride. Do you know of a great paper that uses PF 5274857 hydrochloride from Tocris? Please let us know.
Reviews for PF 5274857 hydrochloride
There are currently no reviews for this product. Be the first to review PF 5274857 hydrochloride and earn rewards!
Have you used PF 5274857 hydrochloride?
Submit a review and receive an Amazon gift card.
$10US/$10CAN/€7/£6 gift card for a review without an image
$25US/$25CAN/€18/£15 gift card for a review with an image
*Offer only valid in the USA / Canada, UK and EuropeSubmit a Review
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.