Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Uprosertib (GSK2141795) 是一种有效的,选择性的 Akt 广谱抑制剂,对 Akt1/Akt2/Akt3 的 IC50值分别为 180/328/38 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 333 | 现货 | ||
2 mg | ¥ 482 | 现货 | ||
5 mg | ¥ 796 | 现货 | ||
10 mg | ¥ 1,280 | 现货 | ||
25 mg | ¥ 2,530 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,730 | 现货 | ||
200 mg | ¥ 6,730 | 现货 | ||
500 mg | ¥ 10,070 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 796 | 现货 |
产品描述 | Uprosertib (GSK2141795) (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2. |
靶点活性 | Akt3:38 nM, Akt2:328 nM, Akt1:180 nM |
体外活性 | Uprosertib inhibits multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cells. Uprosertib preferentially inhibits the proliferation of human cancer cells lines with AKT pathway activation. In LNCaP, BT474, A3 and I9.2 cells lines, Uprosertib also causes cell cycle arrest. [2] In both SKOV3 and PEO4 cells, Uprosertib causes growth-arrest as single agent, and enhances cisplatin-induced apoptosis. [3] |
体内活性 | In mice bearing BT474 breast tumor xenografts, Uprosertib (100 mg/kg, p.o.) results 61% tumor growth inhibition. In mice bearing SKOV3 ovarian tumor xenografts, Uprosertib (30 mg/kg, p.o.) results 61% tumor growth inhibition. [2] |
激酶实验 | Selectivity profiling experiments: The lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or GSK2141795) on an end-over-end shaker for 45 min at 4 °C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4 °C, for both qualitative and quantitative experiments. The beads are washed with 1× CP buffer and collected by centrifugation. Bound proteins are eluted with 2× NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide. |
细胞实验 | Cell lines are typically grown in RPMI 160 medium containing 10% FBS. Some cell lines are grown in media specified by the vendor. A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0–30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.(Only for Reference) |
别名 | GSK2141795, GSK795, 优普色替 |
分子量 | 429.25 |
分子式 | C18H16Cl2F2N4O2 |
CAS No. | 1047634-65-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 76 mg/mL(177.1 mM)
DMSO: 79 mg/mL (184 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.3296 mL | 11.6482 mL | 23.2964 mL | 58.2411 mL |
5 mM | 0.4659 mL | 2.3296 mL | 4.6593 mL | 11.6482 mL | |
10 mM | 0.233 mL | 1.1648 mL | 2.3296 mL | 5.8241 mL | |
20 mM | 0.1165 mL | 0.5824 mL | 1.1648 mL | 2.9121 mL | |
50 mM | 0.0466 mL | 0.233 mL | 0.4659 mL | 1.1648 mL | |
100 mM | 0.0233 mL | 0.1165 mL | 0.233 mL | 0.5824 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Uprosertib 1047634-65-0 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt GSK2141795 GSK-2141795 GSK795 inhibit GSK 795 GSK-795 优普色替 GSK 2141795 Inhibitor PKB Protein kinase B inhibitor