PF-5274857

PF-5274857 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 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway[1].

Product Specifications

CAS Number

[1373615-35-0]

UNSPSC

12352005

Hazard Statement

H317, H319

Target

Smo

Type

Reference compound

Related Pathways

Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer

Assay Protocol

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

Purity

99.31

Solubility

DMSO : 125 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C20H25ClN4O3S

Molecular Weight

436.96

Precautions

H317, H319

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, 11 (1), 57-65.