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PZ0217

Sigma-Aldrich

PF-5274857 hydrochloride

≥98% (HPLC)

Synonym(s):

1-[4-(5′-Chloro-3,5-dimethyl-2,4′-bipyridin-2′-yl)piperazin-1-yl] -3- (methylsulfonyl)propan-1-one hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C20H25ClN4O3S · HCl
CAS Number:
Molecular Weight:
473.42
MDL number:
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: 3 mg/mL, clear (warmed)

storage temp.

room temp

SMILES string

O=C(CCS(C)(=O)=O)N(CC1)CCN1C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2.Cl

InChI

1S/C20H25ClN4O3S.ClH/c1-14-10-15(2)20(23-12-14)16-11-18(22-13-17(16)21)24-5-7-25(8-6-24)19(26)4-9-29(3,27)28;/h10-13H,4-9H2,1-3H3;1H

InChI key

GULNFUQAVPTTQV-UHFFFAOYSA-N

Biochem/physiol Actions

PF-5274857 is a hedgehog (Hh) signaling pathway inhibitor acting as a potent and selective Smoothened (Smo) antagonist with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 completely blocked downstream gene Gli1 transcriptional activity in Gli-Luc mouse embryonic fibroblast (MEF) cells with an IC50 of 2.7 nM. PF-5274857 is brain penetrant. The compound PF-5274857 showed anti-tumor activity in a mouse medulloblastoma model with an in vivo IC50 of 8.9 nM.
PF-5274857 is a hedgehog (Hh) signaling pathway inhibitor acting as a potent and selective Smoothened (Smo) antagonist.

Storage Class

13 - Non Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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