ChemicalBook > CAS DataBase List > pf-5274857

pf-5274857

Product Name
pf-5274857
CAS No.
1373615-35-0
Chemical Name
pf-5274857
Synonyms
CS-601;pf-5274857;PF-5274857 freebase;pf-5274857 USP/EP/BP;PF5274857;PF 5274857;PF-5274857 hydrochloride;PF-5274857;PF 5274857;PF5274857;1-(4-(5-Chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl)piperazin-1-yl)-3-(methylsulfonyl)prop;1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl)-1-piperazinyl]-3-(methylsulfonyl)-1-propanone;1-(4-(5'-Chloro-3,5-dimethyl-[2,4'-bipyridin]-2'-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one
CBNumber
CB62640301
Molecular Formula
C20H25ClN4O3S
Formula Weight
436.96
MOL File
1373615-35-0.mol
More
Less

pf-5274857 Property

storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
H2O: soluble3mg/mL, clear (warmed)
form 
powder
color 
white to beige
More
Less

Safety

WGK Germany 
3
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H317May cause an allergic skin reaction

H319Causes serious eye irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0217
Product name
PF-5274857 hydrochloride
Purity
≥98% (HPLC)
Packaging
5mg
Price
$105
Updated
2022/05/15
Tocris
Product number
5262
Product name
PF-5274857 hydrochloride
Purity
≥98%(HPLC)
Packaging
10
Price
$185
Updated
2021/12/16
TRC
Product number
P293910
Product name
PF-5274857
Packaging
25mg
Price
$310
Updated
2021/12/16
ChemScene
Product number
CS-1206
Product name
PF-5274857
Purity
98.12%
Packaging
5mg
Price
$90
Updated
2021/12/16
ChemScene
Product number
CS-1206
Product name
PF-5274857
Purity
98.12%
Packaging
10mg
Price
$150
Updated
2021/12/16
More
Less

pf-5274857 Chemical Properties,Usage,Production

Uses

PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling, respectively, and can penetrate the blood–brain barrier.

Biological Activity

pf-5274857 is an inhibitor of hedgehog (hh) signaling pathway and is identified as a potent and selective antagonist of smoothened (smo) with an ic50 of 5.8 nm.smoothened, a g protein-coupled receptor, is a component of the hedgehog signaling pathway and is conserved from flies to humans. this protein is the molecular target of the teratogen cyclopamine. smo can act as an oncogene and the activation of smo mutations leads to unregulated activation of the hedgehog pathway and cancer.in mef cells, treatment of pf-5274857 completely blocked shh-induced hh pathway activity, which was measured by the transcriptional activity of smo downstream gene gli1.

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)

in vivo

pf-5274857 showed anti-tumor activity in a mouse medulloblastoma model with ic50 of 8.9 nm. pf-5274857 also shows significant dose-dependent tumor growth inhibition (tgi) and induces tumor regression. in skin tissue, downregulation of gli1 and gli2 is also observed with a similar time course by pf-52748571.

target

Smoothened

References

1. rohner a, spilker me, lam jl, et al. effective targeting of hedgehog signaling in a medulloblastoma model with pf-5274857, a potent and selective smoothened antagonist that penetrates the blood-brain barrier. molecular cancer therapeutics.2012;11(1):57-65.

pf-5274857 Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

pf-5274857 Suppliers

China 68 India 2 The Netherlands 1 United States 14 Global 85
Axon Medchem BV
Tel
--
Fax
--
Email
info@axonmedchem.com
Country
The Netherlands
ProdList
477
Advantage
30
More
Less

View Lastest Price from pf-5274857 manufacturers

Career Henan Chemical Co
Product
pf-5274857 1373615-35-0
Price
US $1.00/KG
Min. Order
1KG
Purity
95%~99%
Supply Ability
per week 100kg
Release date
2019-09-05

1373615-35-0, pf-5274857Related Search:

6-METHYLAMINOPURINE 9-RIBOFURANOSIDE Bortezomib XL765 Lopinavir IOX2 Afatinib

  • pf-5274857
  • PF5274857;PF 5274857
  • CS-601
  • PF-5274857;PF 5274857;PF5274857
  • 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
  • 1-Propanone, 1-[4-(5'-chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl)-1-piperazinyl]-3-(methylsulfonyl)-
  • pf-5274857 USP/EP/BP
  • PF-5274857 freebase
  • 1-(4-(5'-Chloro-3,5-dimethyl-[2,4'-bipyridin]-2'-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one
  • inhibit,driven,PF 5274857,PF5274857,metastasis,pathway,Smo,PF-5274857,Smoothened,Inhibitor,brain,tumor
  • 1-(4-(5'-Chloro-3,5-dimethyl-[2,4'-bipyridin]-2'-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one
  • 1373615-35-0
  • 373615-35-0
  • 73615-35-0
  • C20H25ClN4O3S
  • Inhibitors