PF 5274857 hydrochloride
Cat. No. 5262
Chemical Name: 1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bip
Biological ActivityHigh 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 InformationSold for research purposes under agreement from Pfizer Inc.
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 Data Sheet
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 this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses PF 5274857 hydrochloride from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: PF 5274857 hydrochloride, supplier, PF5274857, hydrochloride, high, affinity, selective, smoothened, Smo, receptor, antagonist, hedgehog, signaling, antitumor, brain, penetrant, orally, available, active, Tocris Bioscience, Smoothened Receptor Antagonist products
Find multiple products by catalog number
New Products in this Area
Selective GPR84 agonistIHR-Cy3
Potent fluorescent Smo antagonistRo 6842262
Potent LPA1 antagonistAMG 853
Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonistAM 4668
Potent FFA1 (GPR40) agonistCATPB
FFA2 antagonist/inverse agonistOleanolic acid
Selective GPBA receptor (TGR5) partial agonistPPTN hydrochloride
High affinity and selective P2Y14 antagonistItraconazole
SMO antagonist; acts at different binding site to cyclopamine (Cat No. 1623)SAR 216471 hydrochloride
Potent P2Y12 antagonist; orally availableA 971432
Potent and selective S1P5 agonistGLPG 0974
Potent FFA2 antagonist
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.