Zanubrutinib (BGB-3111)

A potent and covalent BTK inhibitor

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库存: 现货

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数量
5mg

￥1962.00

1570.00

- +
10mg

￥3487.00

2790.00

- +
25mg

￥6900.00

5520.00

- +
50mg

￥11062.00

8850.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce52392
CAS: 1691249-45-2
别名: 泽布替尼; BGB-3111
分子式: C27H29N5O3
分子量: 471.55
纯度: >98%
溶解度: DMSO : ≥ 56.75 mg/mL (120.35 mM);Ethanol : < 1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Zanubrutinib is a potent and covalent inhibitor of Bruton's tyrosine kinase (BTK; IC₅₀ = 0.3 nM).¹ It is selective for BTK over a panel of 304 kinases at 1 μM but does inhibit EGFR, Tec, Blk, BMX, HER4, and TXK (IC₅₀s = 0.62-33 nM). Zanubrutinib inhibits phosphorylation of BTK at Y233 (IC₅₀ = 1.8 nM) in Ramos cells and reduces viability of REC-1 cells (IC₅₀ = 0.36 nM). In vivo, zanubrutinib (2.5 and 7.5 mg/kg) reduces tumor volume in an OCI-LY10 diffuse large B cell lymphoma (DLBCL) mouse xenograft model.

1.Guo, Y., Liu, Y., Hu, N., et al.Discovery of zanubrutinib (BGB-3111), a novel, potent, and selective covalent inhibitor of bruton's tyrosine kinaseJ. Med. Chem.62(17)7923-7940(2019)