PF-5274857 Inhibitor CAS No. 1373615-35-0

Cat. No.	Name	Size	Price
KI2384	PF-5274857	5 mg	$432
	PF-5274857	10 mg	$752
	PF-5274857	50 mg	$2672
	PF-5274857	100 mg	$3952

Chemical Characteristic

Product Name	PF-5274857
CAS No.	1373615-35-0
Molecular Weight	436.96
Formula	C₂₀H₂₅ClN₄O₃S
Chemical Name	1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one
Smiles	C(=O)(CCS(=O)(=O)C)N1CCN(CC1)c1cc(c(cn1)Cl)c1c(cc(cn1)C)C
Chemical Structure

Biological activities

PF-5274857 is a potent Smoothened (Smo) antagonist. PF-5274857 specifically binds to Smo with a Ki of 4.6 nM. The IC50 of PF-5274857 against Smo is 5.8 nM. PF-5274857 also blocks the transcriptional activity of the downstream gene Gli1 with an IC50 of 2.7 nM in MEF cells. In vivo, PF-5274857 is orally available and metabolically stable. In a mouse model of medulloblastoma in vivo, PF-5274857 has robust antitumor efficacy. In tumor in Ptch+/- p53-/- medulloblastoma allograft mice, PF-5274857 treatment (30 mg/kg) downregulates Gli1, Gli2, Ptch1, and Ptch2 gene expression levels to various degrees. In skin in Ptch+/- p53-/- medulloblastoma allograft mice, PF-5274857 treatment (30 mg/kg) also downregulates Gli1 and Gli2 gene expression. In addition, in the brain of primary medulloblastoma mice, PF-5274857 effectively penetrates the blood-brain barrier and inhibits Smo activity, finally leading to improve animal survival rates.^[1]

Protocols

In vitro and in vivo: PF-5274857 is dissolved in dimethyl sulfoxide for the in vitro assays and formulated in 0.5% methylcellulose for in vivo studies.^[1]

References

[1] Rohner A, 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. Mol Cancer Ther. 2012, 11(1): 57-65.

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