化合物NVP-HDM 201 T5555

Product Introduction
Bioactivity


英文名: Siremadlin

描述: Siremadlin (NVP-HDM 201) 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。

体外活性: Siremadlin有效抑制人类和小鼠的TP53-MDM2相互作用，以纳摩尔级别的细胞IC50值阻止TP53的降解[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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 56.75 mg/mL (102.18 mM)


关键字: HDM 201 | E1/E2/E3 Enzyme | MDM-2/p53 | NVP-HDM-201 | E2 conjugating enzyme | HDM201 | Inhibitor | HDM-201 | Ubiquitin activating enzyme | E3 ligating enzyme | Siremadlin | inhibit | NVP-HDM201 | E1 activating enzyme | Ubiquitin ligase | Ubiquitin conjugating enzyme

相关产品: Nutlin-3a | COH000 | MD-224 | NSC232003 | Cbl-b-IN-10 | NAcM-OPT | Avadomide | RO8994 | M435-1279 | SZL P1-41

相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Lung Cancer Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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