Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD-8835 是选择性的 PI3Kα (IC50:6.2 nM) 和 PI3Kδ (IC50:5.7 nM) 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,080 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 858 | 现货 |
产品描述 | AZD-8835 is a mixed inhibitor of PI3Kα/δ (IC50: 6.2/5.7 nM), also with selectivity against PI3Kβ/γ (IC50: 431/90 nM). |
靶点活性 | PI3Kα:6.2 nM, PI3Kδ:5.7 nM |
体外活性 | AZD8835 is a potent inhibitor of PI3Kα (wild type, E545K and H1047R mutations) and PI3Kδ with excellent selectivity vs. PI3Kβ, PI3Kγ and an excellent general kinase selectivity. AZD8835 is a potent inhibitor of p-Akt in cells sensitive to PI3Kα inhibition (IC50=0.057 μM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50=0.049 μM in JeKo-1 B cell line), but not to cells sensitive to PI3Kβ inhibition (IC50=3.5 μM in PTEN null breast adenocarcinoma MDA-MB-468 cell line) or PI3Kγ inhibition (IC50=0.53 μM in monocytic RAW264 cell line)[2]. |
体内活性 | AZD8835 has antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously and displays high metabolic stability and suitable physical properties for oral administration[1][2]. |
细胞实验 | BT474, MCF7, or T47D cells are seeded in 384-well plates at a density of 500 to 2,000 cells per well and incubated overnight. Cells are dosed with compound(s) and cell confluency is measured at 4-hour intervals over several days.(Only for Reference) |
别名 | AZD8835 |
分子量 | 469.54 |
分子式 | C22H31N9O3 |
CAS No. | 1620576-64-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 86 mg/mL (183.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1297 mL | 10.6487 mL | 21.2974 mL | 53.2436 mL |
5 mM | 0.4259 mL | 2.1297 mL | 4.2595 mL | 10.6487 mL | |
10 mM | 0.213 mL | 1.0649 mL | 2.1297 mL | 5.3244 mL | |
20 mM | 0.1065 mL | 0.5324 mL | 1.0649 mL | 2.6622 mL | |
50 mM | 0.0426 mL | 0.213 mL | 0.4259 mL | 1.0649 mL | |
100 mM | 0.0213 mL | 0.1065 mL | 0.213 mL | 0.5324 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。
AZD-8835 1620576-64-8 PI3K/Akt/mTOR signaling PI3K inhibit AZD 8835 Inhibitor AZD8835 Phosphoinositide 3-kinase inhibitor