产品说明书
Idasanutlin
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同义名 : | RG7388;Ro 5503781 |
| CAS号 : | 1229705-06-9 | |
| 货号 : | A124368 | |
| 分子式 : | C31H29Cl2F2N3O4 | |
| 纯度 : | 99%+ | |
| 分子量 : | 616.482 | |
| MDL号 : | MFCD26142931 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 45 mg/mL(72.99 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear PO 0.5% CMC-Na 60 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tumor suppressor p53 is a powerful growth suppressive and pro-apoptotic protein that plays a central role in protectionfrom tumor development. The overproduction of MDM2, the primary negative regulator of p53, effectively disables p53 function. RG7388, a potent and selective MDM2 antagonist, inhibits p53-MDM2 interaction with an IC50 value of 6 nM. RG7388 induced dose-dependent p53 stabilization, cell cycle arrest, and apoptosis in cancer cells expressing wild-type p53, consistent with a nongenotoxic p53 activation mechanism[2]. In the MDM2-amplified SJSA1 osteosarcoma cell line, a significant apoptotic response over the control was induced with both the single 300 nmol/L and 1.8 μmol/L concentrations of RG7388 for 16 hours (P < 0.005), with the 1.8 μmol/L concentration providing optimal response. In SJSA osteosarcoma xenograft-bearing mice, the once-daily dose of 30 mg/kg of RG7388 (total 210 mg/kg/wk) seemed to be the most effective dose at inhibiting tumor growth (>100% TGI with 9 partial regressions), the 50 mg/kg of RG7388 given twice a week (total 100 mg/kg/wk) was equivalent by statistical analysis (96% TGI with 3 partial regressions; P > 0.05) [1]. It also achieved 88% tumor growth inhibition against established human SJSA1 osterosarcoma xenografts in nude mice at a dose of 12.5 mg/kg[2]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| HCT116 cells | Cytotoxic assay | Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.01 μM | 23808545 | ||
| MDA-MB-435 cells | Cytotoxic assay | Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay, IC50=9.1 μM | 23808545 | ||
| RKO cells | Cytotoxic assay | Cytotoxicity against human RKO cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.07 μM | 23808545 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.62mL 0.32mL 0.16mL |
8.11mL 1.62mL 0.81mL |
16.22mL 3.24mL 1.62mL |
