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GSK2636771 是选择性的、口服有效的PI3Kβ抑制剂,Ki=0.89 nM,IC50=5.2 nM,比p110α和p110γ的选择性高900倍,比p110δ同种型的选择性高10倍。
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GSK2636771 是选择性的、口服有效的PI3Kβ抑制剂,Ki=0.89 nM,IC50=5.2 nM,比p110α和p110γ的选择性高900倍,比p110δ同种型的选择性高10倍。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 413 | 现货 | |
5 mg | ¥ 987 | 现货 | |
10 mg | ¥ 1,550 | 现货 | |
25 mg | ¥ 2,530 | 现货 | |
50 mg | ¥ 3,650 | 现货 | |
100 mg | ¥ 5,390 | 现货 | |
500 mg | ¥ 10,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm. |
靶点活性 | PI3Kβ:5.2 nM |
体外活性 | 在小鼠中,GSK-2636771 (100 mg/kg)不增加葡萄糖/胰岛素水平.在移植瘤模型中,GSK-2636771降低磷酸化的蛋白激酶Akt(Ser473)水平. |
体内活性 | 在PTEN缺失细胞系中,GSK-2636771具有特异的抑制活性,在人前列腺癌PC-3(EC50=36 nM)和乳腺癌HCC70(EC50=72 nM)。 |
细胞实验 | Cells are plated in 96-well microtiter plates at densities ranging from 1,500 to 15,000 cells/well, optimized for untreated control cells to be 80-90% confluent at the endpoint of the experiment. After 24 h, cells are treated with serial dilutions (100pM to 10μM) of GSK2636771. Cell viability is assessed after 72 h of treatment by incubation with CellTiter Blue for 1.5 h. The drug concentration requires for survival of 50% of cells relative to untreated cells (surviving fraction 50, SF50) is determined using GraphPad Prism version 5.0d. Cell lines that fails to achieve the SF50 to a given drug are nominally assigned as the highest concentration screened (i.e. 10μM). At least three independent experiments in triplicate per cell line targeted drug are performed. Association between a mutation and response to a targeted agent is determined using a Fisher’s exact test (GraphPad Prism), and a two-tailed P value <0.05 is considered statistically significant. (Only for Reference) |
别名 | GSK-2636771, GSK 2636771 |
分子量 | 433.42 |
分子式 | C22H22F3N3O3 |
CAS No. | 1372540-25-4 |
Smiles | Cc1nc2c(cc(cc2n1Cc1cccc(c1C)C(F)(F)F)N1CCOCC1)C(O)=O |
密度 | 1.38 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 9 mg/mL (20.77 mM), Sonication is recommended. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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