Alrizomadlin 是一种具有口服活性的 Mdm2 抑制剂，IC50 为 3.8 nM，Ki 分别为 1 nM[1]。 Alrizomadlin 阻断 Mdm2 和 p53 的相互作用，并以 p53 依赖性方式诱导细胞周期停滞和细胞凋亡。

Alrizomadlin is an orally active inhibitor of MDM2 with IC50 of 3.8 nM and Ki of 1 nM, respectively[1]. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

Alrizomadlin (0.001-100 μM) inhibits cell proliferation in a concentration-dependent manner(IC50s: 18.9 nM and 103.5 ± 18.3 nM respectively in AGS and MKN45 cells). Alrizomadlin (0.02-0.2 μM) activates p53 to enhance radiosensitivity in AGS and MKN45 cells and enhances the anti-proliferative effect of radiotherapy at different radiation doses. Stable knockout of p53 abrogates expression of MDM2, p53, p21, PUMA, BAX, Cleaved-caspase3, γH2AX. Alrizomadlin affects progression by inducing cells arrested at G0/G1 phase[3]. Alrizomadlin (0.3 μM-10 μM) leads to a concentration-dependent cell cycle arrest in G2/M phases and decreases S-phase in p53 wide-type cell lines (TPC-1, KTC-1)[4].

In male BALB/c athymic nude mice with MKN45 cells, Alrizomadlin (100 mg/kg; orally) enhances radiation antitumor effect in gastric adenocarcinoma[3].

1818393-16-6

C34H38Cl2FN3O4

642.59

AA-115;APG-115

DMSO:90mg/mL (140.1mM),Need ultrasonic
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In solvent: -80°C for 2 years