PF 5274857 hydrochloride

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Cat.No. 5262 - PF 5274857 hydrochloride | C20H25ClN4O3S.HCl | CAS No. 1613439-62-5
Description: High affinity and selective Smoothened (Smo) receptor antagonist
Chemical Name: 1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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.

Compound Libraries

PF 5274857 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 473.42
Formula C20H25ClN4O3S.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 47.34 100
water 47.34 100

Preparing Stock Solutions

The following data is based on the product molecular weight 473.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Rohner et al (2011) 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 57 PMID: 22084163


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View all Smoothened Receptor Antagonists

Keywords: PF5274857 hydrochloride high affinity selective smoothened Smo receptor antagonist hedgehog signaling antitumor brain penetrant orally available active Smoothened Receptors

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