PF 5274857 hydrochloride

Cat. No. 5262

PF 5274857 hydrochloride C20H25ClN4O3S.HCl [1613439-62-5]

Price and Availability

For PF 5274857 hydrochloride pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride

Biological Activity

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.

Technical Data

M.Wt:
473.42
Formula:
C20H25ClN4O3S.HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
1613439-62-5

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 Datasheet

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 Target

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

Quick Order

Find multiple products by catalog number

divider line

GPCR Product Listing

GPCR Product Listing

Highlights over 450 products for GPCRs. Request copy or view PDF today.

divider line

New Products in this Area

AR-C 69931 tetrasodium salt

Highly potent P2Y12 antagonist

FTY 720

Potent S1P receptor agonist; also immunosuppresent

Cinacalcet hydrochloride

Calcium-sensing receptor (CaSR) allosteric agonist; also CYP2D2 inhibitor and Ca2+ channel blocker; orally bioavailable

AMG 837 hemicalcium salt

Potent free fatty acid receptor 1 (FFA1/GPR40) partial agonist

UMB 68

GHB receptor ligand

AZD 1283

High affinity P2Y12 antagonist

Ex 26

Potent and selective S1P1 receptor antagonist

ZQ 16

Selective GPR84 agonist

IHR-Cy3

Potent fluorescent Smo antagonist

Ro 6842262

Potent LPA1 antagonist

AMG 853

Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist

AM 4668

Potent FFA1 (GPR40) agonist

CATPB

FFA2 antagonist/inverse agonist

Sign-up for new product e-alerts
divider line

LinkedIn Updates

Follow Tocris on LinkedIn

Follow us on LinkedIn!

Visit our LinkedIn page for the latest Tocris news, events and updates.