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Siremadlin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Siremadlin图片
CAS NO:1448867-41-1
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
NVP-HDM 201
产品介绍
Siremadlin 是一种有效的、可口服的、高度特异性的 p53-Mdm2 相互作用抑制剂。

产品描述

Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.

体外活性

Siremadlin inhibits both human and murine TP53- MDM2 interactions, with nanomolar cellular IC50 values, blocking TP53 degradation[1]

体内活性

Tumors are allografted in large cohorts of mice to assess the pharmacologic effects of Siremadlin (NVP-HDM201). Sixteen out of 21 allograft models are sensitive to Siremadlin (NVP-HDM201) but ultimately relapse under treatment[1]. Siremadlin has recently entered Phase 1 clinical trials in cancer patients[2]. Siremadlin (NVP-HDM201) administered either daily at a low dose or once at a high dose revealed a differentiated engagement of the p53 molecular response. In contrast to the daily low dose treatment regimen, the single high dose Siremadlin (NVP-HDM201) regimen results in a rapid and dramatic induction of p53-dependent PUMA expression and apoptosis. This is consistent with the finding that a single high dose Siremadlin (NVP-HDM201) treatment, administered orally or intravenously, results in a robust and sustained tumor regression. Overall, both daily and once every 3 weeks dosing regimen shows comparable long term efficacy in preclinical studies. The ongoing clinical trial is currently designed to compare both dosing regimens with regard to efficacy and tolerability[3].

Cas No.

1448867-41-1

分子式

C26H24Cl2N6O4

分子量

555.42

别名

NVP-HDM 201

储存和溶解度

DMSO:56.75 mg/mL (102.18 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years