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首页-抗体药物偶连体和PROTACs-PROTAC-BGB-16673
BGB-16673

Chemical Structure : BGB-16673

CAS No.: 2736508-94-2

BGB-16673 (BGB16673)

货号: PC-21567Not For Human Use, Lab Use Only.

BGB-16673 is an orally available heterobifunctional BTK PROTAC degrader that binds to BTK and E3 ligase, degrades wildtype BTK and multiple mutant forms via ubiquitination.

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纯度 & COA & 质检文件 纯度: 99.7% (HPLC) Select Batch:

生物&药学活性

BGB-16673 is an orally available heterobifunctional BTK PROTAC degrader that binds to BTK and E3 ligase, degrades wildtype BTK and multiple mutant forms via ubiquitination.
BGB-16673 exhibits high potency on clinically relevant BTK mutants resistant to covalent and non-covalent BTK inhibitors in cancer cells in vitro.
BGB-16673 drives complete tumor regression of lymphoma xenograft models expressing wildtype or BTK mutations resistant to covalent and non-covalent inhibitors.
BGB-16673 presents longer duration of response than BTK inhibitors in BTK wildtype and C481S mutant-expressing lymphoma xenograft models.

物理化学性质&存储条件

分子量 850.04
分子式 C48H55N11O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(tert-butyl)-N-((1R)-1-(4-(6-(6-(4-((1-(4-(2,6-dioxopiperidin-3-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)pyridin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2-methylphenyl)ethyl)-1,2,4-oxadiazole-5-carboxamide

参考文献

1. John F. Seymour, et al. Blood (2023) 142 (Supplement 1): 4401.

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