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Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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10 mM * 1 mL/5 mg/10 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1270.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥843.0 |
| 规格： | 10 mg | 产品价格： | ￥1350.0 |
| 规格： | 50 mg | 产品价格： | ￥3450.0 |
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GSK1904529A
CAS No. : 1089283-49-7
MCE 国际站：GSK1904529A
产品活性：GSK1904529A 是一种有效的，选择性的，具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体 (IGF-1R) 和胰岛素受体 (IR) 抑制剂，IC50 值分别为 27 和 25 nM。GSK1904529A 在其他 45 种丝氨酸/苏氨酸和酪氨酸激酶中显示出较弱的活性 (IC50>1 μM)。GSK1904529A 具有抗肿瘤活性。
研究领域：Protein Tyrosine Kinase/RTK | Apoptosis
作用靶点：IGF-1R | Insulin Receptor | Apoptosis
In Vitro: GSK1904529A displays high affinities for IGF-1R and IR, with Kis of 1.6 and 1.3 nM, respectively.
GSK1904529A (72 h) inhibits tumor cells proliferation with IC50s ranges from 35 nM to >30 μM, and Ewing's sarcoma and multiple myeloma cell lines are greatest sensitive.
GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle.
GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC50s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively.
GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR cells.
In Vivo: GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice.
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice.
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice.
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文献和实验【翻译】Development trends for monoclonal antibody cancer therapeutics
two murine, Y-90 ibritumomab tiuxetan (Zevalin; Biogen Idec) and I-131 tositumomab (Bexxar; Corixa/GSK), and one chimeric, I-131 ch-TNT (Shanghai Medipharm Biotech) — have been approved for non-Hodgkin's lymphoma or lung cancer, but only 14% of anticancer
【转帖】2011年中国工程院院士增选进入第二轮评审的候选人名单
最大的制药企业葛兰素史克公司（NYSE: GSK）完成收购Reliant药业公司，收购价为16.5亿美元 更多阅读 --> （各学部名单按照姓名拼音排序） 中国工程院2011年院士增选第一轮评审工作已经结束，各学部经过候选人材料审阅、专业组评审、全学部评审和投票等程序（其中工程管理学部候选人在相关背景学部进行评审），从485位有效候选人中产生了进入第二轮评审的候选人163位，根据《中国工程院院士增选工作实施办法》的规定，现予以公布
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