Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Afuresertib (GSK2110183) 是一个选择性,ATP 竞争性,口服有效的泛 Akt 抑制剂,作用于 Akt1、Akt2和 Akt3,Ki 值分别为 0.08、2、2.6 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
2 mg | ¥ 448 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,370 | 现货 | ||
25 mg | ¥ 2,560 | 现货 | ||
50 mg | ¥ 3,790 | 现货 | ||
100 mg | ¥ 5,470 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 982 | 现货 |
产品描述 | Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. |
靶点活性 | Akt1:0.08 nM(Ki), Akt2:2 nM(Ki), Akt3:2.6 nM(Ki) |
体外活性 | 用10,30和100 mg/kg Afuresertib处理负荷SKOV3卵巢肿瘤异种移植物的小鼠,分别导致凝血酶形成指数为23%,37%和97%.每天给负荷BT474乳腺肿瘤异种移植物的小鼠,口服10,30或100 mg/kg Afuresertib,分别导致凝血酶形成指数为8%,37%和61%. |
体内活性 | 总体上65%的血液学细胞系对Afuresertib敏感,EC50 < 1 μM。在测试的实体肿瘤细胞系中,21%对Afuresertib的EC50 <1 μM。Afuresertib抑制E17K AKT1突变蛋白的激酶活性,EC50为0.2 nM。Afuresertib显示对多种AKT底物磷酸化水平(包括GSK3b,PRAS40,FOXO和胱天蛋白酶9)的浓度依赖性效应。 |
激酶实验 | Potency (Ki*) of afuresertib: The true potency (Ki*) of the inhibitor is initially determined at low enzyme concentrations (0.1 nM AKT1, 0.7 nM AKT2, and 0.2 nM AKT3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSS-FAEPG-amide) and [γ33P] ATP. Reactions are terminated after 2 h and the radio labeled AKT peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2). |
细胞实验 | 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 | GSK2110183C, GSK2110183 |
分子量 | 427.32 |
分子式 | C18H17Cl2FN4OS |
CAS No. | 1047644-62-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 79 mg/mL (184.9 mM)
Ethanol: 79 mg/mL (184.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.3402 mL | 11.7008 mL | 23.4017 mL | 58.5042 mL |
5 mM | 0.468 mL | 2.3402 mL | 4.6803 mL | 11.7008 mL | |
10 mM | 0.234 mL | 1.1701 mL | 2.3402 mL | 5.8504 mL | |
20 mM | 0.117 mL | 0.585 mL | 1.1701 mL | 2.9252 mL | |
50 mM | 0.0468 mL | 0.234 mL | 0.468 mL | 1.1701 mL | |
100 mM | 0.0234 mL | 0.117 mL | 0.234 mL | 0.585 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。
Afuresertib 1047644-62-1 Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling PI3K/Akt/mTOR signaling Stem Cells ROCK Akt PKC ROK Rho-associated kinase Rho-kinase Inhibitor Rho-associated protein kinase GSK-2110183 GSK2110183C inhibit PKB GSK 2110183 GSK2110183 Protein kinase C Protein kinase B inhibitor