Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zanubrutinib (BGB-3111) 是 Bruton tyrosine kinase(Btk) 的选择性抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 595 | 现货 | ||
2 mg | ¥ 863 | 现货 | ||
5 mg | ¥ 1,420 | 现货 | ||
10 mg | ¥ 2,560 | 现货 | ||
25 mg | ¥ 4,280 | 现货 | ||
50 mg | ¥ 6,130 | 现货 | ||
100 mg | ¥ 8,450 | 现货 | ||
500 mg | ¥ 16,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK). |
体外活性 | In both biochemical and cellular assays, BGB-3111 demonstrated nanomolar BTK inhibition activity. In several MCL and DLBCL cell lines, BGB-3111 inhibited BCR aggregation-triggered BTK autophosphorylation, blocked downstream PLC-γ2 signaling, and potently inhibited cell proliferation. In comparison with ibrutinib, BGB-3111 showed much more restricted off-target activities against a panel of kinases, including ITK. While ibrutinib significantly inhibited rituximab-induced NK cell IFN-γ secretion and in vitro cytotoxicity on mantle cell lymphoma cells, BGB-3111 was at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity[1]. |
体内活性 | In mouse BTK occupancy assays, treatment with BGB-3111 resulted in a dose-dependent BTK occupancy and showed about 3-fold more potency than ibrutinib in target organs, including PBMC and spleen.?BGB-3111 induced dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice.?In the subcutaneous xenografts, BGB-3111 at 2.5 mg/kg BID showed similar activity as ibrutinib at 50 mg/kg QD, its clinical relevant dose.?In the systemic model, the median survival of BGB-3111 25 mg/kg BID group was significantly longer than those of both ibrutinib 50 mg/kg QD and BID groups.?In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, BGB-3111 also demonstrated better anti-tumor activity than ibrutinib.?Preliminary 14-day toxicity study in rats showed that BGB-3111 was very well tolerated and maximal tolerate dose (MTD) was not reached when it was dosed up to 250mg/kg/day[1]. |
别名 | 赞鲁替尼, BGB-3111, 泽布替尼 |
分子量 | 471.55 |
分子式 | C27H29N5O3 |
CAS No. | 1691249-45-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 56.75 mg/mL (120.35 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1207 mL | 10.6033 mL | 21.2067 mL | 53.0166 mL |
5 mM | 0.4241 mL | 2.1207 mL | 4.2413 mL | 10.6033 mL | |
10 mM | 0.2121 mL | 1.0603 mL | 2.1207 mL | 5.3017 mL | |
20 mM | 0.106 mL | 0.5302 mL | 1.0603 mL | 2.6508 mL | |
50 mM | 0.0424 mL | 0.2121 mL | 0.4241 mL | 1.0603 mL | |
100 mM | 0.0212 mL | 0.106 mL | 0.2121 mL | 0.5302 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。
zanubrutinib 1691249-45-2 Angiogenesis Tyrosine Kinase/Adaptors BTK 赞鲁替尼 Btk BGB3111 BGB-3111 泽布替尼 Inhibitor BGB 3111 inhibit Bruton tyrosine kinase inhibitor