Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 是一种选择性和 ATP 竞争性的泛 I 类 PI3K 抑制剂。它具有优越的抗肿瘤活性,对除 mTOR 以外的其他脂质和蛋白激酶的选择性也超过 2,000 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 459 | 现货 | ||
2 mg | ¥ 667 | 现货 | ||
5 mg | ¥ 997 | 现货 | ||
10 mg | ¥ 1,530 | 现货 | ||
25 mg | ¥ 2,580 | 现货 | ||
50 mg | ¥ 3,870 | 现货 | ||
100 mg | ¥ 5,530 | 现货 |
产品描述 | Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor (IC50s: 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ). Copanlisib dihydrochloride has superior antitumor activity and it also has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. |
靶点活性 | mTOR:45 nM, PI3Kγ:6.4 nM, PI3Kα:0.5 nM, PI3Kβ:3.7 nM, PI3Kδ:0.7 nM |
体外活性 | In both KPL4 cells and LPA-stimulated PC3 cells, BAY 80-6946 reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, BAY 80-6946 shows antiproliferative activity and induces apoptosis. [1] The combination of HER2-targeted therapies and BAY 80-6946 inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells. [2] |
体内活性 | In rat KPL4 or HCT116 tumor xenograft model, BAY 80-6946 (6 mg/kg, i.v.) induces 100% complete tumor regression. In nude mice with Lu7860 erlotinib-resistant, patient-derived NSCLC and MAXF1398 patient-derived luminal breast tumor models, BAY 80-6946 (14 mg/kg, i.v.) also causes tumor growth inhibition. [1] |
别名 | 库潘尼西盐酸, BAY 80-6946 dihydrochloride |
分子量 | 553.44 |
分子式 | C23H30Cl2N8O4 |
CAS No. | 1402152-13-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mM
H2O: 20 mg/mL, Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8069 mL | 9.0344 mL | 18.0688 mL | 45.172 mL |
5 mM | 0.3614 mL | 1.8069 mL | 3.6138 mL | 9.0344 mL | |
10 mM | 0.1807 mL | 0.9034 mL | 1.8069 mL | 4.5172 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。
Copanlisib dihydrochloride 1402152-13-9 Apoptosis PI3K/Akt/mTOR signaling PI3K mTOR Inhibitor antiproliferative inhibit intravenous 库潘尼西盐酸 BAY 80-6946 sub-nanomolar Copanlisib BAY 80-6946 dihydrochloride BAY 80-6946 Dihydrochloride phosphorylation Copanlisib Dihydrochloride Phosphoinositide 3-kinase AKT antitumor administration inhibitor