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SAR405838  ≥95%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥ 50 mg/mL）
产品描述：基本信息 产品编号：S10734 产品名称：SAR405838 CAS: 1303607-60-4   储存条件 粉末 -20℃ 四年     分子式： C29H34Cl2FN3O3 溶于液体 -80℃ 六个月 分子量 562.50 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 100mg/mL (177.77mM) Ethanol 31mg/mL warmed with 50ºC water bath (55.11mM) Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.7778mL 8.8889mL 17.7778mL 5mM 0.3556mL 1.7778mL 3.5556mL 10mM 0.1778mL 0.8889mL 1.7778mL 50mM 0.0356mL 0.1778mL 0.3556mL   生物活性 产品描述 一种高效的选择性MDM2抑制剂, 与MDM2结合, Ki值为0.88nM。 靶点/IC50 p53 MDM2SAR405838 (MI-77301) potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092μM), RS4;11 (IC50,0.089μM),LNCaP (IC50, 0.27μM), and HCT-116 (IC50, 0.20μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10μM), PC-3 (IC50,>10μM),SW620 (IC50, >10μM), and HCT-116 (p53-/-)(IC50,>20μM) cells.SAR405838 effectively induces apoptosis in the RS4;11 cell line. SAR405838 potently inhibits cell growth and induces dosedependent apoptosis in the ABTR1 and ABTR2 sublines, albeit with modestly reduced potency compared with that in the control RS4;11 cell line.(Cell-free assay)   0.88nM(Ki) 体外研究 SAR405838 (MI-77301) potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50,0.092μM),RS4;11 (IC50,0.089μM),LNCaP (IC50, 0.27μM), and HCT-116 (IC50, 0.20μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10μM), PC-3 (IC50,>10μM),SW620 (IC50, >10μM), and HCT-116 (p53-/-)(IC50,>20μM) cells.SAR405838 effectively induces apoptosis in the RS4;11 cell line. SAR405838 potently inhibits cell growth and induces dosedependent apoptosis in the ABTR1 and ABTR2 sublines, albeit with modestly reduced potency compared with that in the control RS4;11 cell line. 体内研究 At well-tolerated dose schedules, SAR405838 achieves either durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia,LNCaP prostate cancer and HCT-116 colon cancer.Remarkably, a single oral dose of SAR405838 is sufficient to achieve complete tumor regression in the SJSA-1 model.In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10mg/kg, 30mg/kg, 50mg/kg, 100mg/kg, and 200mg/kg,).   推荐实验方法(仅供参考) 激酶实验： 荧光偏振结合法 使用荧光偏振结合法检测MDM2抑制剂和p53肽与MDM2蛋白的亲和性；MI-773与Bcl-2、Bcl-xL、Mcl-1和 β-catenin的亲和性用竞争性荧光偏振结合法检测；与MDMx的亲和性用BioLayer干涉技术检测。   细胞实验:   细胞系 SJSA-1、RS4;11、LNCaP、SAOS-2、PC-3、SW620、HCT-116和HCT-116(p53-/-)细胞系 浓度 100μM 处理时间 ~48 小时 方法 细胞增殖抑制实验用水溶性四氮唑盐法检测，细胞死亡用台盼蓝染色法检测。   动物实验:   动物模型 负荷SJSA-1骨肉瘤、RS4;11急性淋巴细胞白血病和HCT-116结肠癌的雌性SCID小鼠，负荷LNCaP前列腺癌的雄性SCID小鼠。 剂量 ~200毫克/千克 给药处理 口服给药
保存条件：-20℃

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