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Idasanutlin {[allProObj[0].p_purity_real_show]}

货号:A124368 同义名: RG7388;Ro 5503781

Idasanutlin (RG7388) 是一种强效且选择性的 MDM2 拮抗剂,IC50 为 6 nM,能抑制 p53-MDM2 结合。

Idasanutlin 化学结构 CAS号:1229705-06-9
Idasanutlin 化学结构
CAS号:1229705-06-9
Idasanutlin 3D分子结构
CAS号:1229705-06-9
Idasanutlin 化学结构 CAS号:1229705-06-9
Idasanutlin 3D分子结构 CAS号:1229705-06-9
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Idasanutlin 纯度/质量文件 产品仅供科研

货号:A124368 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 p53 其他靶点 纯度
Pifithrin-μ 99%+
Pifithrin-α HBr 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Idasanutlin 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].

Idasanutlin 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
SJSA1 cells Cytotoxic assay Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.01 μM 23808545

Idasanutlin 实验方案

计算器
存储液制备 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

Idasanutlin 技术信息

CAS号1229705-06-9
分子式C31H29Cl2F2N3O4
分子量 616.482
别名 RG7388;Ro 5503781
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

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

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