(±)-Zanubrutinib (Synonyms: (±)-泽布替尼; (±)-BGB-3111)
目录号: PL01231 纯度: ≥99%
CAS No. :1633350-06-7
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中文名称
(±)-Zanubrutinib
英文名称
(±)-Zanubrutinib
英文别名
7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide;BGB3111;(+/-)-Zanubrutinib;((plusmn))-Zanubrutinib;2-(4-phenoxyphenyl)-7-(1-prop-2-enoylpiperidin-4-yl)-1,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide;BDBM249900;BCP25045;BCP25838;NSC799318;SB18877;( inverted exclamation markA)-Zanubrutinib;US9447106, 27;C(C=C)(=O)N1CCC(CC1)C1CCNC=2N1N=C(C;(±)-Zanubrutinib
Cas No.
1633350-06-7
分子式
C27H29N5O3
分子量
471.55
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
(±)-Zanubrutinib ((±)-BGB-3111) 是一种有效选择性的,具有口服活性的 Bruton's 酪氨酸激酶 (Btk) 抑制剂。
生物活性
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Brutons tyrosine kinase (Btk) inhibitor.
性状
Solid
体外研究(In Vitro)
In both biochemical and cellular assays, (±)-Zanubrutinib ((±)-BGB-3111) 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 PCI-32765, (±)-Zanubrutinib shows much more restricted off-target activities against a panel of kinases, including ITK. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(±)-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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Na L, et al. BGB-3111 is a novel and highly selective Brutons 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): A
溶解度数据
In Vitro: DMSO : ≥ 30 mg/mL (63.62 mM)Ethanol : ≥ 10 mg/mL (21.21 mM)
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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