Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Alrizomadlin (APG-115) 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 2,660 | 现货 | ||
2 mg | ¥ 3,810 | 现货 | ||
5 mg | ¥ 6,120 | 现货 | ||
10 mg | ¥ 8,430 | 现货 | ||
25 mg | ¥ 12,500 | 现货 | ||
50 mg | ¥ 16,800 | 现货 | ||
100 mg | ¥ 22,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 7,720 | 现货 |
产品描述 | 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. |
靶点活性 | APG-115:3.8 nM |
体外活性 | 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]. |
体内活性 | In male BALB/c athymic nude mice with MKN45 cells, Alrizomadlin (100 mg/kg; orally) enhances radiation antitumor effect in gastric adenocarcinoma[3]. |
别名 | 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: 90mg/mL (140.1mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5562 mL | 7.781 mL | 15.562 mL | 38.9051 mL |
5 mM | 0.3112 mL | 1.5562 mL | 3.1124 mL | 7.781 mL | |
10 mM | 0.1556 mL | 0.7781 mL | 1.5562 mL | 3.8905 mL | |
20 mM | 0.0778 mL | 0.3891 mL | 0.7781 mL | 1.9453 mL | |
50 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7781 mL | |
100 mM | 0.0156 mL | 0.0778 mL | 0.1556 mL | 0.3891 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Alrizomadlin 1818393-16-6 Apoptosis Mdm2 AA 115 APG-115 APG115 AA115 APG 115 AA-115 Inhibitor inhibitor inhibit