Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and <100-fold selectivity over all other bromodomains.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,530 | 5日内发货 | ||
25 mg | ¥ 11,700 | 8-10周 | ||
50 mg | ¥ 15,200 | 8-10周 | ||
100 mg | ¥ 21,500 | 8-10周 |
产品描述 | BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. |
靶点活性 | BAZ2B:180 nM, BAZ2A:170 nM(kd), BAZ2A:130 nM, BAZ2A:(kd)109 nM |
体外活性 | To investigate whether BAZ2-ICR (Compound 13) can displace BAZ2 bromodomains from chromatin in living cells. A fluorescence recovery after photobleaching (FRAP) assay utilizing GFP-tagged BAZ2A full length protein transfected into human osteosarcoma cells (U2OS) are tested. 1 μM BAZ2-ICR reduces the recovery time of the wild-type (wt) construct to a level similar to the dominant negative mutant, confirming that BAZ2-ICR inhibits BAZ2A in cells[1]. |
体内活性 | BAZ2-ICR (5 mg/kg) shows 70% bioavailability and moderate clearance (~50% of mouse liver blood flow) and volume of distribution[1]. BAZ2-ICR (Compound 13) shows very high solubility (25 mM in D2O), a measured log D of 1.05. High stability in mouse microsomes, and permeation in the CaCo-2 model and thus a suitable profile for oral and intravenous gavage. |
分子量 | 357.41 |
分子式 | C20H19N7 |
CAS No. | 1665195-94-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
BAZ2-ICR 1665195-94-7 Chromatin/Epigenetic Epigenetic Reader Domain BAZ2ICR BAZ-2-ICR BAZ2 ICR Inhibitor inhibitor inhibit