Tocris/PF 5274857 hydrochloride/5262/10/10 mg-蚂蚁淘生物

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) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

High affinity and selective Smoothened (Smo) receptor antagonist (K_i = 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.

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

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

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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