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zanubrutinib

zanubrutinib

产品编号 T7584   CAS 1691249-45-2
别名: 赞鲁替尼, BGB-3111, 泽布替尼

Zanubrutinib (BGB-3111) 是 Bruton tyrosine kinase(Btk) 的选择性抑制剂。

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zanubrutinib Chemical Structure
zanubrutinib, CAS 1691249-45-2
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
其他形式的 zanubrutinib:
产品目录号及名称: zanubrutinib (T7584)
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选择批次  
纯度: 99.74%
纯度: 99.24%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 56.75 mg/mL (120.35 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Li N , Sun Z , Liu Y , et al. Abstract 2597: BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor[J]. Cancer Research, 2015, 75(15 Supplement):2597-2597. 2. Chiara Tarantelli, Lu Zhang, Elisabetta Curti ,et al.The Bruton Tyrosine Kinase Inhibitor Zanubrutinib (BGB-3111) Demonstrated Synergies With Other Anti-Lymphoma Targeted Agents[J].Haematologica, 104 (7), e307-e309 Jul 2019
GDC-0834 SB-633825 TAK-020 (Rac)-IBT6A BTK-IN-27 PROTAC BTK Degrader-5 CHMFL-BTK-01 DBt-10

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 高选择性抑制剂库 抗癌上市药物库 抗癌临床化合物库 酪氨酸激酶分子库 抗癌药物库 经典已知活性库 口服活性化合物库 血液病分子库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

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

 

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