Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
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1 mg | 在庫あり | ¥ 14,000 | |||
5 mg | 在庫あり | ¥ 30,500 | |||
10 mg | 在庫あり | ¥ 45,500 | |||
25 mg | 在庫あり | ¥ 83,000 | |||
50 mg | 在庫あり | ¥ 136,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 38,000 |
説明 | Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor. |
In vitro | Siremadlin inhibits both human and murine TP53- MDM2 interactions, with nanomolar cellular IC50 values, blocking TP53 degradation[1] |
In vivo | 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]. |
別名 | NVP-HDM 201 |
分子量 | 555.41 |
分子式 | C26H24Cl2N6O4 |
CAS No. | 1448867-41-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 56.75 mg/mL (102.18 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Siremadlin 1448867-41-1 Ubiquitination E1/E2/E3 Enzyme HDM 201 MDM-2/p53 NVP-HDM-201 E2 conjugating enzyme HDM201 Inhibitor HDM-201 NVP-HDM 201 Ubiquitin activating enzyme E3 ligating enzyme inhibit NVP-HDM201 E1 activating enzyme Ubiquitin ligase Ubiquitin conjugating enzyme inhibitor