Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mivebresib (ABBV-075) 是一种有效的,口服活性的溴结构域和末端结构域 (BET) 抑制剂,结合BRD4的Ki 值是 1.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
2 mg | ¥ 589 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,590 | 现货 | ||
25 mg | ¥ 3,280 | 现货 | ||
50 mg | ¥ 4,820 | 现货 | ||
100 mg | ¥ 6,690 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 917 | 现货 |
产品描述 | Mivebresib (ABBV-075), also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins. |
靶点活性 | BET:1.5 nM(ki) |
体外活性 | ABBV-075 exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit[1]. |
体内活性 | ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia[1]. |
别名 | ABBV-075, 米维布塞 |
分子量 | 459.47 |
分子式 | C22H19F2N3O4S |
CAS No. | 1445993-26-9 |
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: 84 mg/mL (183 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1764 mL | 10.8821 mL | 21.7642 mL | 54.4105 mL |
5 mM | 0.4353 mL | 2.1764 mL | 4.3528 mL | 10.8821 mL | |
10 mM | 0.2176 mL | 1.0882 mL | 2.1764 mL | 5.4411 mL | |
20 mM | 0.1088 mL | 0.5441 mL | 1.0882 mL | 2.7205 mL | |
50 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0882 mL | |
100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5441 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。
Mivebresib 1445993-26-9 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain ABBV-075 ABBV 075 ABBV075 Inhibitor 米维布塞 inhibit inhibitor