(±)-Zanubrutinib
作者：齊岳
發布時間：2023-08-23
09:17:18
點擊數：
產品名稱：(±)-Zanubrutinib
產品描述：
| 產品描述 | (±)-Zanubrutinib is a potent and orally available Bruton's tyrosine kinase (Btk) inhibitor that demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibi. |
| 體外活性 | In both biochemical and cellular assays, (±)-Zanubrutinib demonstrates nanomolar Btk inhibition activity. In comparison with ibrutinib, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK. In several MCL and DLBCL cell lines, (±)-Zanubrutinib inhibits BCR aggregation-triggered Btk autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation[1]. |
| 體內活性 | (±)-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 a very well tolerated and maximally tolerated dose (MTD) is not reached when it is dosed up to 250mg/kg/day[1]. |
| 別名 | (±)-BGB-3111 |
| 分子量 | 471.55 |
| 分子式 | C27H29N5O3 |
| CAS No. | 1633350-06-7 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 27.0 mg/mL (57.3 mM)
Ethanol: 9.0 mg/mL (19.1 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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