Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vistusertib (AZD2014) 是一种ATP 竞争性的mTOR 抑制剂,IC50为 2.81 nM。它抑制mTORC1和mTORC2复合物。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 377 | 现货 | ||
5 mg | ¥ 573 | 现货 | ||
10 mg | ¥ 956 | 现货 | ||
25 mg | ¥ 1,681 | 现货 | ||
50 mg | ¥ 2,480 | 现货 | ||
100 mg | ¥ 3,997 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 627 | 现货 |
产品描述 | Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. |
靶点活性 | pS6 (S235/236):200 nM, mTOR:2.8 nM, pAkt (S473):80 nM |
体外活性 | 在人类ER+乳腺癌移植模型中,AZD2014通过调控mTORC1和mTORC2底物,抑制肿瘤生长. |
体内活性 | 在乳腺癌细胞系(抗激素疗法的ER+细胞系)中,AZD2014抑制细胞生长,促使细胞凋亡。AZD2014能够抑制mTORC2的生物标记pAKTSer473和 pNDRG1Thr346。 |
激酶实验 | Recombinant truncated FLAG-tagged mTOR expressed in HEK 293 cells is used in biochemical assays, together with a biotinylated p70S6K peptide substrate. Streptavidin donor and protein A acceptor beads are used to assemble the capture complex for generation of the assay signal. The activity of the lipid kinases, PI3K alpha, beta, delta, and gamma are measured using recombinant proteins and the lipid PIP2 as substrate. Assays for ATM and DNA-PK activity are performed. The mTOR cellular activity is measured in MDAMB468 cells, using an Acumen laser scanning cytometer to analyze the levels of phosphorylation of S6 (Ser235/236) and AKT (Ser473)[1]. |
细胞实验 | AZD2014 is prepared in DMSO (10 mM) and stored under nitrogen, and then diluted with appropriate media before use[1]. Cells are plated in 96-well plates for the indicated time. For CellTiterGlo assays: CellTiterGlo is mixed with the cells. Cells are normalized to day 0 control and net growth is determined using the following formula: ((x?y)/(z?y))=net growth, where x=reading of treated sample at end of study, y=average reading on day 0, and z=reading of DMSO-treated sample at end of study. The concentration of DMSO does not exceed 0.03% for any experiment. For MTS assays: adherent cell lines are grown in 96-well plates. MTS reagent is added on day 0 and on day 3 post-AZD2014 addition. Suspension lines are assayed using the Alamar Blue reagent, 72 hours after AZD2014 addition[1]. |
别名 | AZD2014 |
分子量 | 462.54 |
分子式 | C25H30N6O3 |
CAS No. | 1009298-59-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 36 mg/mL (77.8 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.162 mL | 10.8099 mL | 21.6198 mL | 54.0494 mL |
5 mM | 0.4324 mL | 2.162 mL | 4.324 mL | 10.8099 mL | |
10 mM | 0.2162 mL | 1.081 mL | 2.162 mL | 5.4049 mL | |
20 mM | 0.1081 mL | 0.5405 mL | 1.081 mL | 2.7025 mL | |
50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.081 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。
Vistusertib 1009298-59-2 Apoptosis Autophagy Cytoskeletal Signaling MAPK PI3K/Akt/mTOR signaling Akt PI3K S6 Kinase mTOR AZD2014 inhibit AZD-2014 Mammalian target of Rapamycin AZD 2014 Inhibitor inhibitor