PF 5274857 hydrochloride

Cat. No. 5262 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： High affinity and selective Smoothened (Smo) receptor antagonist

化学名： 1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride

纯度： ≥98% (HPLC)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for PF 5274857 hydrochloride

PF 5274857 hydrochloride is a 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.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for PF 5274857 hydrochloride

PF 5274857 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for PF 5274857 hydrochloride

分子量	473.42
公式	C₂₀H₂₅ClN₄O₃S.HCl
储存	Desiccate at RT
纯度	≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PF 5274857 hydrochloride

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	47.34	100
	DMSO	47.34	100

制备储备液 for PF 5274857 hydrochloride

以下数据基于产品分子量 473.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	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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产品说明书 for PF 5274857 hydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PF 5274857 hydrochloride

参考文献是支持产品生物活性的出版物。

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

If you know of a relevant reference for PF 5274857 hydrochloride, please let us know.

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