CAS No. 1373615-35-0

Batch: Purity:99.86
PF-5274857 Chemical Structure
Chemical Structure
Check the PF-5274857 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Chemical Information

CAS Number 1373615-35-0
Molecular Formula

C20H25ClN4O3S

Molecular Weight (MW) 436.96
SMILES CC1=CC(=C(N=C1)C2=CC(=NC=C2Cl)N3CCN(CC3)C(=O)CCS(=O)(=O)C)C

Biological Activity

PF-5274857 is a potent, orally bioavailable, and brain-penetrant Smoothened (Smo) antagonist that inhibits Hedgehog pathway signaling with an IC50 of 2.7 nM and a Ki of 4.6 nM. By selectively targeting Smo, PF-5274857 suppresses downstream transcriptional targets such as Gli1 and Ptch1, leading to impaired Hh-driven cell proliferation and significant tumor regression in preclinical medulloblastoma models. [1]

How to Prepare Stock Solution?

Concentration Volume Mass
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Solubility

Batch:
All in vitro solubility values are batch-tested experimental data (non-literature values).
Solvent Solubility & Note
DMSO 93 mg/mL (212.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.)
Water 93 mg/mL
Ethanol Insoluble
FAQ
Q: Why does a DMSO stock precipitate in media/saline?
A: It is caused by unheated aqueous media (supersaturation), local solvent shock, or incorrect mixing sequence.
How to fix it?
  • Preheat media/saline to 37°C.
  • Mix rapidly (pipette/vortex) upon addition.
  • For complex mixes, always add the aqueous phase last.
  • Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).

Reference

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Note: Technical data last updated: Sep 1, 2026.