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PF-5274857 (hydrochloride)

PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway[1].

Product Specifications

CAS Number

1613439-62-5

UNSPSC

12352005

Target

Smo

Type

Reference compound

Related Pathways

Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pf-5274857-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C(N1CCN(C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2)CC1)CCS(=O)(C)=O.Cl

Molecular Formula

C20H26Cl2N4O3S

Molecular Weight

473.42

References & Citations

[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 Jan;11 (1) :57-65.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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