pf-5274857

Mary031

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pf-5274857 Basic information

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Product Name:

pf-5274857

Synonyms:

pf-5274857;1-(4-(5-chloro-4-(3,5-diMethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(Methylsulfonyl)propan-1-one;1-[4-(5′-Chloro-3,5-dimethyl-2,4′-bipyridin-2′-yl)piperazin-1-yl] -3- (methylsulfonyl)propan-1-one hydrochloride;PF-5274857 hydrochloride;1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl)-1-piperazinyl]-3-(methylsulfonyl)-1-propanone;1-(4-(5-Chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)prop

CAS:

1373615-35-0

MF:

C20H25ClN4O3S

MW:

436.9555

EINECS:

-0

Product Categories:

-;Inhibitors

Mol File:

1373615-35-0.mol

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pf-5274857 Usage And Synthesis

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Enzyme inhibitor

This brain-penetrating Smoothened (Smo) antagonist (FW = 436.96 g/mol; CAS 1373615-35-0), also known as 1-(4-(5-chloro-4-(3,5-dimethylpyridin- 2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one, potentlyand selectively inhibits Hedgehog (Hh) signaling (IC50 = 5.8 nM; Ki = 4.6 nM). PF-5274857 elicits robust antitumor activity in a mouse model of medulloblastoma (IC50 = 8.9 nmol/L), with down-regulation of Gli1, a marker closely linked to the tumor growth inhibition in patched (+/-) medulloblastoma mice. PF-5274857 also inhibits Smo activity within the brain of primary medulloblastoma mice, improving survival. PF-5274857 is orally available and metabolically stable in vivo. Other Hedgehog inhibitors include: GANT61, BMS-833923, Purmorphamine, SANT-1, LY2940680, Cyclopamine, LDE225 (or NVP-LDE225, Erismodegib), Vismodegib (GDC-0449)

Product Name	pf-5274857
CAS No	1373615-35-0
EC-No	200-204-2
Min. Order	1KG
Purity	95%~99%
Release date	2019/09/06

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