PF 5274857 hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 5262
High affinity and selective Smoothened (Smo) receptor antagonist
Key Product Details
Description
High affinity and selective Smoothened (Smo) receptor antagonist
Product Description
PF 5274857 hydrochloride is a high affinity and selective Smoothened (Smo) receptor antagonist (Ki = 4.6 nM). Exhibits >1000-fold selectivity for Smo over a panel of other receptors, ion channels and enzymes. Inhibits Shh-induced Hedgehog signaling in MEF cells. Induces tumor regression in a medulloblastoma allograft mouse model. Orally available and brain penetrant.Licensing Information
Sold for research purposes under agreement from Pfizer Inc.Product Specifications
Molecular Weight
473.42
Formula
C20H25ClN4O3S.HCl
Storage
Desiccate at RT
Purity
≥98% (HPLC)
Chemical Name
1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride
CAS Number
1613439-62-5
PubChem ID
90489027
InChI Key
GULNFUQAVPTTQV-UHFFFAOYSA-N
SMILES
CC1=CN=C(C2=CC(N3CCN(C(CCS(C)(=O)=O)=O)CC3)=NC=C2Cl)C(C)=C1.Cl
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 47.34 | 100 | |
| DMSO | 47.34 | 100 |
Preparing Stock Solutions
for PF 5274857 hydrochloride
The following data is based on the product molecular weight 473.42
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.11 mL | 10.56 mL | 21.12 mL |
| 5 mM | 0.42 mL | 2.11 mL | 4.22 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.11 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Rohner 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. 2011 PMID: 22084163
Product Specific Notices for PF 5274857 hydrochloride
For research use only
Loading...
Loading...