Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VE-821 (ATR Inhibitor IV) 是一种有效的 ATP 竞争性的ATR 抑制剂,Ki 为 13 nM,IC50为 26 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 415 | 现货 | ||
10 mg | ¥ 697 | 现货 | ||
25 mg | ¥ 1,259 | 现货 | ||
50 mg | ¥ 1,996 | 现货 | ||
100 mg | ¥ 3,717 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 457 | 现货 |
产品描述 | VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki/IC50: 13/26 nM in cell-free assays). |
靶点活性 | ATR:13 nM (Ki, cell free) |
体外活性 | VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-dependent protein kinase (DNA-PK), mammalian target of rapamycin and phosphoinositol 3-kinase-γ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively). VE-821 blocked H2AX phosphorylation in hydroxyurea-treated HT29 cancer cells and had no impact on the M059J or HT144 lines treated with neocarzinostatin [1]. VE-821 significantly enhanced the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 led to inhibition of radiation-induced G 2/M arrest in cancer cells [2]. VE-821 (1 and 4 μM) enhanced H2AX phosphorylation on Ser139 induced by topotecan, and cisplatin in OVCAR-8 cells. VE-821 did not block ATR-mediated Ser345 Chk1 or Ser296 autophosphorylation triggered by gemcitabine, topotecan, or cisplatin [3]. |
激酶实验 | The ability of compounds (e.g., VE-821) to inhibit ATR, ATM or DNAPK kinase activity is tested using a radiometric-phosphate incorporation assay. A stock solution is prepared consisting of the appropriate buffer, kinase, and target peptide. To this is added the compound of interest, at varying concentrations in DMSO to a final DMSO concentration of 7%. Assays are initiated by addition of an appropriate [g-33P]ATP solution and incubated at 25°C. Assays are stopped, after the desired time course, by addition of phosphoric acid and ATP to a final concentration of 100 mM and 0.66 μM, respectively. Peptides are captured on a phosphocellulose membrane, prepared, and washed six times with 200 μL of 100 mM phosphoric acid, prior to the addition of 100 μL of scintillation cocktail and scintillation counting on a 1450 Microbeta Liquid Scintillation Counter. Dose-response data are analyzed using GraphPad Prism software [4]. |
细胞实验 | Clonogenic survival assays were performed as described before. Briefly, logarithmically growing cells were plated in triplicate in 6-well tissue culture dishes under oxic (21% O2) or hypoxic conditions (0.5% O2) using an InVivo2 300 chamber. Cells were incubated for 6 h before irradiation under oxia or hypoxia using tightly sealed chambers. The target O2 level was achieved within 6 h of gassing and maintained during irradiation, as confirmed by an OxyLite oxygen probe. Cells irradiated under hypoxia were exposed to normoxia at 1 h post-irradiation. As standard, VE-821 (1 μM) was added 1 h prior to irradiation (6 Gy) and was washed away 72 h after irradiation. For the chemotherapy experiments, cells were initially exposed to increasing concentrations of gemcitabine (5, 10 and 20 nM) for 24 h before addition of the VE-821 (1 μM) for another 72 h. The effect of triple combination of irradiation with VE-821 and gemcitabine was examined as well. Cells were incubated for 10–21 d until colonies were stained with 0.5% crystal violet and counted in a CellCount automated colony counter. Clonogenic survival was calculated and data were fitted in GraphPad Prism 4.0 [2]. |
别名 | ATR Inhibitor IV |
分子量 | 368.41 |
分子式 | C18H16N4O3S |
CAS No. | 1232410-49-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 69 mg/mL (187.3 mM)
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 | 2.7144 mL | 13.5718 mL | 27.1437 mL | 67.8592 mL |
5 mM | 0.5429 mL | 2.7144 mL | 5.4287 mL | 13.5718 mL | |
10 mM | 0.2714 mL | 1.3572 mL | 2.7144 mL | 6.7859 mL | |
20 mM | 0.1357 mL | 0.6786 mL | 1.3572 mL | 3.393 mL | |
50 mM | 0.0543 mL | 0.2714 mL | 0.5429 mL | 1.3572 mL | |
100 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6786 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。
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