Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Alrizomadlin (APG-115) 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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 60,500 |
2 mg | 在庫あり | ¥ 86,500 |
5 mg | 在庫あり | ¥ 143,000 |
10 mg | 在庫あり | ¥ 204,000 |
25 mg | 在庫あり | ¥ 305,500 |
50 mg | 在庫あり | ¥ 411,000 |
100 mg | 在庫あり | ¥ 558,000 |
500 mg | 在庫あり | ¥ 1,120,000 |
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 180,500 |
説明 | Alrizomadlin (APG-115) 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. |
ターゲット&IC50 | MDM2:3.8 nM |
In vitro | 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 vivo | In male BALB/c athymic nude mice with MKN45 cells, Alrizomadlin (100 mg/kg; orally) enhances radiation antitumor effect in gastric adenocarcinoma[3]. |
別名 | APG-115, AA-115 |
分子量 | 642.59 |
分子式 | C34H38Cl2FN3O4 |
CAS No. | 1818393-16-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (140.1 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Alrizomadlin 1818393-16-6 Apoptosis Mdm2 AA 115 APG-115 APG115 AA115 APG 115 AA-115 Inhibitor inhibitor inhibit