(±)-Zanubrutinib 也称为 (±)-BGB-3111,是一种有效的、选择性的口服 BTK 抑制剂,表现出纳摩尔级的 BTK 抑制活性。
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产品名称 | BTK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
CGI-1746 |
+++
BTK, IC50: 1.9 nM |
98% | |||||||||||||||||
Spebrutinib |
++++
BTK, IC50: <0.5 nM |
98+% | |||||||||||||||||
Acalabrutinib |
++
BTK, IC50: 3nM |
98% | |||||||||||||||||
CNX-774 |
+++
BTK, IC50: <1 nM |
99%+ | |||||||||||||||||
Ibrutinib |
++++
BTK, IC50: 0.5 nM |
98% | |||||||||||||||||
ONO-4059 analog |
+
BTK, IC50: 23.9 nM |
98% | |||||||||||||||||
RN486 |
++
BTK, IC50: 4 nM |
99%+ | |||||||||||||||||
(Z)-LFM-A13 |
+
BTK, Ki: 1.4 μM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | (±)-Zanubrutinib, also known as (±)-BGB-3111, is an efficacious, selective, oral Btk inhibitor that exhibits nanomolar-level Btk inhibitory activity. In various MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR-triggered autophosphorylation of Btk, blocks downstream PLC-γ2 signaling, and effectively suppresses cell proliferation. Compared to PCI-32765, (±)-Zanubrutinib demonstrates more restricted off-target activity against a panel of kinases, including ITK[1]. |
Animal study | In the REC-1 MCL xenograft animal model, either subcutaneously or systemically transplanted, (±)-Zanubrutinib induces a dose-dependent antitumor effect through intravenous injection via the tail vein. A preliminary 14-day toxicity study in rats with subcutaneous xenografts showed excellent tolerance for (±)-Zanubrutinib, with doses up to 250 mg/kg/day without reaching the maximum tolerated dose[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.12mL 0.42mL 0.21mL |
10.60mL 2.12mL 1.06mL |
21.21mL 4.24mL 2.12mL |
CAS号 | 1633350-06-7 |
分子式 | C27H29N5O3 |
分子量 | 471.551 |
别名 | (±)-BGB-3111 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 30 mg/mL(63.62 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 8 mg/mL(16.97 mM),注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 |
动物实验配方 |