A Smo antagonist
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PF-5274857

Item No. 43595

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-(5′-chloro-3,5-dimethyl[2,4′-bipyridin]-2′-yl)-1- piperazinyl]-3-(methylsulfonyl)-1-propanone
CAS Number
1373615-35-0
Molecular Formula
C20H25ClN4O3S
Formula Weight
437.0
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CS(=O)(CCC(N1CCN(CC1)C2=NC=C(Cl)C(C3=C(C=C(C=N3)C)C)=C2)=O)=O
InChi Code
InChI=1S/C20H25ClN4O3S/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
InChi Key
BBVNTTZIOTWDSV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $58

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    10 mg

    $109

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    50 mg

    $487

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    100 mg

    $801

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    Cayman Chemical
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    Product Description

    PF-5274857 is a smoothened receptor (Smo) antagonist.1 It binds to Smo (Ki = 4.6 nM) and inhibits transcription of Gli1 in mouse embryonic fibroblasts (MEFs; IC50 = 2.7 nM). In vivo, PF-5274857 inhibits tumor growth and induces tumor regression in a medulloblastoma mouse allograft model when administered at doses less than 10 mg/kg and greater than 10 mg/kg, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rohner, A., Spilker, M.E., Lam, J.L., 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. 11(1), 57-65 (2012).