LOGIN IN
REGISTER
PRODUCTS
More than 5000 active chemicals with high quality for research!

Email sales@dcchemicals.com

        order@dcchemicals.com

        info@dcchemicals.com


Phone:  +86-21-58447131

Fax   +86-21-61642470

PF-5274857
DC12373  (CAS:1373615-35-0)
(Based on popularity)
Size Price Availability
100mg USD 600 in stock
250mg USD 1100 in stock
1g USD 2200 in stock
We match the best price and quality on market.
 
 
Email: order@dcchemicals.com
Tel: +86-21-58447131
Fax:+86-21-61642470
Fields of Application :
PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the bloodCbrain barrier.
CAS Number: 1373615-35-0
Purity:

>98%

Molecular Weight: 436.96
Molecular Formula: C20H25ClN4O3S
Quality Control: HPLCNMR LC/MS(Please contact us to get the QC report)
Synonyms: PF-5274857,PF 5274857,PF5274857
Chemical Name:
Storage: 2 years -20C Powder, 2 weeks4C in DMSO,6 months-80C in DMSO
Note: Products for research use only, not for human use
Description:
PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the bloodCbrain barrier. IC50 value: 5.8 nM Target: Smoothened in vitro: PF-5274857 completely inhibits Shh-induced Hh pathway activity with IC50 of 2.7 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells. The -opioid receptor is weakly inhibited by PF-5274857 with a dissociation constant of 36 M subsequently determined in a functional assay [1]. in vivo: PF-5274857 shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression at high doses(>10 mg/kg)., PF-5274857 downregulates Gli1, Gli2, Ptch1, and Ptch2 gene expression levels to various degrees with maximal effects being achieved between 6 and 12 hours post-dose (Gli1 is the most sensitive gene), whereas PF-5274857 has little effect on Smo levels. In skin tissue, downregulation of Gli1 and Gli2 is also observed with a similar time course by PF-5274857. The model-derived drug concentration for half maximal inhibition of the tumor Gli1 mRNA production rate (IC50) by PF-5274857 is determined to be 8.9 nM in the Ptch+/?p53+/? medulloblastoma allograft mice, which mathematically corresponds to tumor regression of 119% TGI after 6 days of plasma exposure at this concentration. In the Ptch+/?p53?/? medulloblastoma allograft mice, the IC50 value is estimated to be 3.5 nM, consistent with the Ptch+/?p53+/? results. PF-5274857 is also able to cross the bloodCbrain barrier in rats within 4 hours post-dose.
References:
O=C(N1CCN(C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2)CC1)CCS(=O)(C)=O
About us Products Services ordering sitemap
Phone: +86-21-58447131Fax: +86-21-61642470
ADDRoom 610, Building 15, Jinxiang Rd 201, Pudong,Shanghai, China
CopyRight-2010-2013 DC Chemicals All Rights Reserved