(±)-Zanubrutinib ((±)-BGB-3111)

(±)-Zanubrutinib ((±)-BGB-3111) ((±)-BGB-3111) 是一种有效的、选择性的和口服的 Bruton's 酪氨酸激酶 (Btk) 抑制剂。

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库存: 现货

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数量
1mg

￥475.00

380.00

- +
5mg

￥1062.00

850.00

- +
10mg

￥1687.00

1350.00

- +
50mg

￥5037.00

4030.00

- +

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货号: ajce52380
CAS: 1633350-06-7
别名: (±)-赞鲁替尼,(±)-BGB-3111
分子式: C27H29N5O3
分子量: 471.55
纯度: >98%
溶解度: DMSO : ≥ 30 mg/mL (63.62 mM);Ethanol : ≥ 10 mg/mL (21.21 mM)
储存: Store at -20°C
库存: 现货

Background

(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.

In both biochemical and cellular assays, (±)-Zanubrutinib demonstrates nanomolar Btk inhibition activity. In several MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. In comparison with ibrutinib, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK. (±)-Zanubrutinib is at least 10-fold weaker than ibrutinib in inhibiting rituximab induced ADCC, consistent with its weak ITK inhibition activity[1].

(±)-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 subcutaneous xenografts. 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 250mg/kg/day[1].

[1]. Na L, et al. BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2597. doi:10.1158/1538-7445.AM2015-2597