Zanubrutinib (BGB-3111) (Synonyms: BGB-3111) |
Catalog No.GC34075 |
자누브루티닙(BGB-3111)(BGB-3111)은 선택적 브루톤 티로신 키나제(Btk) 억제제입니다.
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Cas No.: 1691249-45-2
Sample solution is provided at 25 µL, 10mM.
Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
Zanubrutinib (BGB-3111) is a selective Bruton 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[1].
Zanubrutinib (BGB-3111) 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, Zanubrutinib at 2.5 mg/kg BID shows similar activity as ibrutinib at 50 mg/kg QD. In the systemic model, the median survival of Zanubrutinib 25 mg/kg BID group is significantly longer than those of both ibrutinib 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 ibrutinib. 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].
[1]. Na Li, et al. Abstract 2597: BGB-3111 is a novel and highly selective Bruton's tyrosine kinase (BTK) inhibitor. Cancer Res 2015;75(15 Suppl):Abstract nr 2597.
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