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产品介绍
产品介绍
产品信息
抗原名称
p53/MDM2 interaction

商品描述
HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.

分子量
555.41

纯度
>98%

可溶性
DMSO : ≥ 56.75 mg/mL (102.18 mM)

外观
Powder

In vitro(体外研究)
HDM201 binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction of the two proteins and leading to the activation of the p53 pathway. It induces robust p53-dependent cell cycle arrest and apoptosis in human p53 wild-type tumor cells. HDM201 exhibits highly selectivity across a panel of cancer cell lines.

In vivo(体内研究)
HDM201 displays desirable pharmacokinetic and pharmacodynamic profiles in animals together with excellent oral bioavailability. Application of the compound using various dosing schedules triggers rapid and sustained activation of p53-dependent pharmacodynamic biomarkers resulting in tumor regression in multiple xenografted models of p53 wild-type human cancers.

背景
别名
NVP-HDM201;HDM-201;NVP-HDM-201

分子式
C26H24Cl2N6O4

CAS号
1448867-41-1

制备和贮存
保存方式
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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