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NSC781406  ≥98%

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包装规格：1mg 5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(150mg/mL超声）
产品描述：基本信息 产品编号： N11404 产品名称： NSC781406 CAS: 1676893-24-5   储存条件 粉末 -20℃ 四年     分子式： C29H27F2N5O5S2 溶于液体 -80℃ 6个月 分子量： 627.68 -20℃ 1个月 化学名：  2,4-Difluoro-N-[2-methoxy-5-[4-[3-(4-methylsulfonylpiperazin-1-yl)prop-1-ynyl]quinolin-6-yl]pyridin-3-yl]benzenesulfonamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   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 1.5932mL 7.9658mL 15.9317mL 5mM 0.3186mL 1.5932mL 3.1863mL 10mM 0.1593mL 0.7966mL 1.5932mL   生物活性 产品描述 一种高效的PI3K和mTOR抑制剂，对PI3Kα的IC50值为2nM。 靶点 PI3K;mTOR 体外研究 NSC781406 demonstrates potent PI3K inhibition (PI3KαIC50=2.0nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20nM).NSC781406 displays reasonable liver microsome stability.NSC781406 demonstrates cytotoxic activities against leukemia,non-small cell,lung cancer,colon cancer,central nervous system cancer,melanoma,ovarian cancer,renal cancer,prostate cancer,and breast cancer.It is potent against 60 cancer cell lines with a mean GI50 value of 65nM,and with a GI50 value less than 10nM against four cancer cell lines. 体内研究 In the xenograft models, treatment with 30mg/kg of NSC781406 results in statistically significant antitumor activity,with a mean reduction in relative tumor volume ratio of 52%.Sorafenib displays an inhibition ratio of 44% at 50mg/kg.NSC781406 is well tolerated at 30mg/kg,with no observed mortality or significant reduction of body weight.   推荐实验方法(仅供参考) 激酶实验： IC50 values for inhibition of the PI3K is measured.PI-103 is used as the reference compound.The compounds (NSC781406) are tested in duplicate for 10 concentrations,100nM or 500nM as the top concentration.All reagents are diluted in kinase buffer.Three-fold,ten-point serial compound (NSC781406) dilutions are performed in kinase buffer.   细胞实验:   Cytotoxic effects are tested in the human lung adenocarcinoma cells A549,human colon cancer cells HCT-116,human breast cancer cells MDA-MB-231 and human hepatocellular carcinoma cells BEL-7404.These four tumor cells are diluted to a density of 40,000–50,000 cells/mL in logarithmic phase.After the cells are treated with compounds (NSC781406) for 72h,MTT solution (5mg/mL,20μL) is added another 4h at 37℃.IC50 values are determined by a nonlinear regression analysis.   动物实验:   Mice:NSC781406 is orally administered once a day 30mg/kg for 14 consecutive days or with sorafenib at 50mg/kg.The relative tumor volume to vehicle-treated control mice is monitored.
保存条件：-20℃

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