| 中文名称: | NSC781406 | ||||
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| 英文名称: | NSC781406 | ||||
| 别名: | NSC781406 2,4-Difluoro-N-[2-methoxy-5-[4-[3-(4-methylsulfonylpiperazin-1-yl)prop-1-ynyl]quinolin-6-yl]pyridin-3-yl]benzenesulfonamide | ||||
| CAS No: | 1676893-24-5 | 分子式: | C29H27F2N5O5S2 | 分子量: | 627.68 |
| CAS No: | 1676893-24-5 | ||||
| 分子式: | C29H27F2N5O5S2 | ||||
| 分子量: | 627.68 | ||||
基本信息
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产品编号： |
N11404 |
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产品名称： |
NSC781406 |
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CAS: |
1676893-24-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
627.68 |
-20℃ |
1个月 |
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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 |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.5932mL |
7.9658mL |
15.9317mL |
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5mM |
0.3186mL |
1.5932mL |
3.1863mL |
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10mM |
0.1593mL |
0.7966mL |
1.5932mL |
生物活性
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产品描述 |
一种高效的PI3K和mTOR抑制剂，对PI3Kα的IC50值为2nM。 |
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靶点 |
PI3K;mTOR |
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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. |
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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)
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激酶实验： |
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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. |
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细胞实验: |
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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. |
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动物实验: |
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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. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
