Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ARV-825 是一种双功能 PROTAC,蛋白水解靶向嵌合体,将 BRD4 募集到 E3 泛素连接酶大脑中,导致 BRD4 在所有测试的 BL 细胞系中快速、有效和延长降解。对 BRD4 的 BD1 和 BD2 结构域具有高亲和力,Kd 值分别为 90 和 28 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 456 | 现货 | ||
2 mg | ¥ 645 | 现货 | ||
5 mg | ¥ 996 | 现货 | ||
10 mg | ¥ 1,680 | 现货 | ||
25 mg | ¥ 2,990 | 现货 | ||
50 mg | ¥ 4,390 | 现货 | ||
100 mg | ¥ 6,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,690 | 现货 |
产品描述 | ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested. |
靶点活性 | BRD4 BD2:28 nM (Kd), BRD4 BD1:90 nM (Kd) |
体外活性 | ARV-825 more effectively suppresses c-MYC levels and downstream signaling than small molecule BRD4 inhibitors resulting in more effective cell proliferation inhibition and apoptosis induction in BL.In Burkitt's lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis. |
细胞实验 | Cells (50000/100ul) were seeded in 96-well tissue culture plates followed by addition of ARV-825?at indicated concentration.?After 72 hours, 100 μL per well of reconstituted CellTiter-Glo reagent was added and read on Cytation 3 imaging reader.?Relative cell growth was determined by comparing assay readings of treated cells with control DMSO treated cells.?For apoptosis induction, Caspase-Glo 3/7 Assay was used following manufacturer s instruction. |
分子量 | 923.43 |
分子式 | C46H47ClN8O9S |
CAS No. | 1818885-28-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (54.15 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.0829 mL | 5.4146 mL | 10.8292 mL | 27.073 mL |
5 mM | 0.2166 mL | 1.0829 mL | 2.1658 mL | 5.4146 mL | |
10 mM | 0.1083 mL | 0.5415 mL | 1.0829 mL | 2.7073 mL | |
20 mM | 0.0541 mL | 0.2707 mL | 0.5415 mL | 1.3536 mL | |
50 mM | 0.0217 mL | 0.1083 mL | 0.2166 mL | 0.5415 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。
ARV-825 1818885-28-7 Chromatin/Epigenetic Epigenetic Reader Domain ARV 825 inhibit PROTACs Inhibitor ARV825 inhibitor