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首页-抗体药物偶连体和PROTACs-PROTAC-CDK6 PROTAC CP-10
CDK6 PROTAC CP-10

Chemical Structure : CDK6 PROTAC CP-10

CAS No.: 2366268-80-4

CDK6 PROTAC CP-10

货号: PC-26501Not For Human Use, Lab Use Only.

CDK6 PROTAC CP-10 is a potent, selective CDK6 degrader (DC50=2.1 nM, U251 cells) generated by linking CDK6 inhibitor palbociclib and E3 ligase CRBN recruiter pomalidomide.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CDK6 PROTAC CP-10 is a potent, selective CDK6 degrader (DC50=2.1 nM, U251 cells) generated by linking CDK6 inhibitor palbociclib and E3 ligase CRBN recruiter pomalidomide.
CP-10 induces specific degradation of CDK6, with far weaker CDK4 degradation with DC50 of 150-180 nM.
CP-10 induces degradation of CDK6 by the ubiquitin-proteasome system.
CP-10 shows cell inhibition potential (IC50=10 nM) in multiple myeloma cell MM.lS and mantle cell lymphoma cells (in Mino, IC50=8 nM) or comparable activities in leukemia cells, induces degradation of amplified/mutated forms of CDK6 (D163G mutation).

物理化学性质&存储条件

分子量 871.96
分子式 C44H49N13O7
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

4-((2-(2-(4-((4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

参考文献

1. Shang Su, et al. J Med Chem. 2019 Aug 22;62(16):7575-7582.

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