PZ0217
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
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
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
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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