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CAS No. : 1818393-16-6
MCE 国际站:Alrizomadlin
产品活性:Alrizomadlin (APG-115) 是一种口服活性小分子 MDM2 蛋白抑制剂, 可与 MDM2 蛋白结合,IC50 值和 Ki 值分别为3.8 nM 和 1 nM。Alrizomadlin 可阻断 MDM2 与 p53 的相互作用并且以 p53 依赖性方式诱导细胞周期停滞和凋亡 (apoptosis)。
研究领域:Apoptosis | Metabolic Enzyme/Protease
作用靶点:MDM-2/p53 | E1/E2/E3 Enzyme | Apoptosis
In Vitro: Alrizomadlin (0.001-100 μM; 72 hours) inhibits cell proliferation in concentration-dependent manner, with IC50s of 18.9 ± 15.6 nM and 103.5 ± 18.3 nM respectively in AGS and MKN45 cells. Alrizomadlin (0.02 μM, 0.2 μM; 48 hours) enhances the anti-proliferative effect of radiotherapy at different radiation dose. Alrizomadlin (0.02 μM, 0.2 μM; 48 hours) affects progression by inducing cells arrested at G0/G1 phase in AGS and MKN45 cell with wild p53. Alrizomadlin (0.02 μM, 0.2 μM; 24 hours) activates p53 to enhance radiosensitivity in AGS and MKN45 cells; stable knockout of p53 abrogates expression of MDM2, p53, p21, PUMA, BAX, Cleaved-caspase3, γH2AX. Alrizomadlin (0.3 μM, 1 μM, 3 μM, 10 μM; 24 hours) leads to a concentration-dependent cell cycle arrest in G2/M phases and a decreasing in S-phase in p53 wide-type cell lines (TPC-1, KTC-1).
In Vivo: Alrizomadlin (Delivered orally; 100 mg/kg; once daily; 10 days) enhances radiation antitumor effect in gastric adenocarcinoma in vivo.
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货号: HY-101518
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