Zanubrutinib

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Chemical Structure| 1691249-45-2 同义名 : 赞鲁替尼 ;BGB-3111
CAS号 : 1691249-45-2
货号 : A702104
分子式 : C27H29N5O3
纯度 : 99%+
分子量 : 471.551
MDL号 : MFCD31567461
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 190 mg/mL(402.93 mM)，配合低频超声助溶，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
动物实验配方：
生物活性
描述 Bruton’s tyrosine kinase (BTK), an essential component of the B-cell antigen receptor (BCR) pathway, has emerged as novel target in the treatment of B-cell malignancies . Zanubrutinib is a selective BTK inhibitor. It demonstrates nanomolar BTK inhibition activity in both biochemical and cellular assays. In several MCL and DLBCL cell lines, Zanubrutinib inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. Zanubrutinib induces dose-dependent anti-tumor effects against REC-1 MCL xenografts engrafted either subcutaneously or systemically via tail vein injection in mice. In the systemic model, the median survival of Zanubrutinib 25 mg/kg BID group is significantly longer than those of both PCI-32765 50 mg/kg QD and BID groups. In an ABC-subtype DLBCL (TMD-8) subcutaneous xenograft model, Zanubrutinib also demonstrates better anti-tumor activity than PCI-32765. Preliminary 14-day toxicity study in rats shows that Zanubrutinib is very well tolerated and maximal tolerate dose (MTD) is not reached when it is dosed up to 250 mg/kg/day .[1]
作用机制 Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
实验方案
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