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CAS No.: 1691249-45-2

Zanubrutinib/泽布替尼 Catalog No. CSN22147

Synonyms: BGB-3111;Brukinsa;泽布替尼

Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

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技术信息

生物活性

描述Bruton's tyrosine kinase (BTK), an essential component of the B-cell antigen receptor (BCR) pathway, has emerged as novel target in the treatment of B-cell malignancies . Zanubrutinib is a selective BTK inhibitor. It demonstrates nanomolar BTK inhibition activity in both biochemical and cellular assays. In several MCL and DLBCL cell lines, Zanubrutinib inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation. 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 systemic model, the median survival of Zanubrutinib 25 mg/kg BID group is significantly longer than those of both PCI-32765 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 PCI-32765. 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]
作用机制Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03740529	Chronic Lymphocytic Leukemia ... more >> Waldenstrom's Macroglobulinemia Mantle Cell Lymphoma Marginal Zone Lymphoma B-cell Lymphoma Small Lymphocytic Lymphoma Collapse <<	Phase 1 Phase 2	Recruiting	April 2021	United States, Tennessee ... more >> Sarah Cannon Research Institute at Tennessee Oncology Recruiting Nashville, Tennessee, United States, 37203 Contact: Ian W Flinn, MD, PhD Collapse <<
NCT03053440	Waldenström's Macroglobulinemi... more >>a Collapse <<	Phase 3	Active, not recruiting	June 2021	-
NCT03432884	Healthy Volunteers	Phase 1	Completed	-	United States, New Jersey ... more >> Frontage Clinical Services, Inc. Secaucus, New Jersey, United States, 07094 Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1207 mL
- 10.6033 mL
- 21.2066 mL
- 5 mM
- 0.4241 mL
- 2.1207 mL
- 4.2413 mL
- 10 mM
- 0.2121 mL
- 1.0603 mL
- 2.1207 mL

技术信息

CAS号

1691249-45-2

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H29N5O3

运输

蓝冰

分子量

471.55

别名

BGB-3111;Brukinsa;泽布替尼

溶解度

DMSO	112.5 mg/mL (238.6 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03740529	Chronic Lymphocytic Leukemia ... more >> Waldenstrom's Macroglobulinemia Mantle Cell Lymphoma Marginal Zone Lymphoma B-cell Lymphoma Small Lymphocytic Lymphoma Collapse <<	Phase 1 Phase 2	Recruiting	April 2021	United States, Tennessee ... more >> Sarah Cannon Research Institute at Tennessee Oncology Recruiting Nashville, Tennessee, United States, 37203 Contact: Ian W Flinn, MD, PhD Collapse <<
NCT03053440	Waldenström's Macroglobulinemi... more >>a Collapse <<	Phase 3	Active, not recruiting	June 2021	-
NCT03432884	Healthy Volunteers	Phase 1	Completed	-	United States, New Jersey ... more >> Frontage Clinical Services, Inc. Secaucus, New Jersey, United States, 07094 Collapse <<
NCT03465059	Hepatic Insufficiency & Health... more >>y Subjects Collapse <<	Phase 1	Active, not recruiting	December 2018	United States, Florida ... more >> University of Miami Miami, Florida, United States, 33124 Orlando Clinical Research Center Orlando, Florida, United States, 32809 Collapse <<
NCT03734016	Chronic Lymphocytic Leukemia ... more >> Small Lymphocytic Lymphoma Collapse <<	Phase 3	Recruiting	October 2025	United States, Nevada ... more >> Comprehensive Cancer Centers of Nevada - USOR Recruiting Las Vegas, Nevada, United States, 89169 Principal Investigator: Edwin Kingsley, MD United States, New Jersey Summit Medical Group Recruiting Florham Park, New Jersey, United States, 07932 Principal Investigator: Charles Farber, MD United States, New York Clinical Research Alliance Inc Recruiting Lake Success, New York, United States, 11042 Principal Investigator: Morton Coleman, MD United States, Washington Medical Oncology Associates Recruiting Spokane, Washington, United States, 99208 Principal Investigator: Arvind Chaudhry Collapse <<
NCT03561298	Healthy Subjects	Phase 1	Completed	-	United States, Florida ... more >> Covance Clinical Research Unit Daytona Beach, Florida, United States, 32117 Collapse <<

Zanubrutinib/泽布替尼 Catalog No. CSN22147

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