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首页-抗体药物偶连体和PROTACs-PROTAC-DDO3602
DDO3602

Chemical Structure : DDO3602

CAS No.:

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DDO3602 (DDO-3602)

货号: PC-25824Not For Human Use, Lab Use Only.

DDO3602 is a potent, effective small molecule HSP90-mediated proteolysis-targeting chimera (HSPTAC) degrader of PARP1 with DC50 of 490.3 nM in MCF-7 cells, induces PARP1 degradation through a multi-E3 ubiquitin ligase-mediated degradation pathway.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DDO3602 is a potent, effective small molecule HSP90-mediated proteolysis-targeting chimera (HSPTAC) degrader of PARP1 with DC50 of 490.3 nM in MCF-7 cells, induces PARP1 degradation through a multi-E3 ubiquitin ligase-mediated degradation pathway.
DDO3602 effectively degrades PARP1 levels by 69.7% at a concentration of 1 μM.
DDO3602 exhibits significant MCF-7 antiproliferative activity (IC50 = 187 nM) for MCF-7 cells.
DDO3602 recruits multiple E3 ubiquitin ligases, including such as tripartite motif-containing protein 25 (TRIM25), ubiquitin protein ligase 5 (UBR5), Myc-binding protein 2 (MYCBP2), membrane-associated RING finger protein 5 (MARCHF5), and tripartite motif-containing protein 50 (TRIM50), thereby promoting PARP1 degradation via a UPS-dependent manner.
DDO3602 effectively induces G2/M cell cycle arrest and DNA damage.
DDO3602 inhibits the migration of MCF-7 cells and exhibits effective anticancer activity in the MCF-7 xenograft tumor mouse model.

物理化学性质&存储条件

分子量 900.07
分子式 C51H58FN7O7
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

1-(4-((2-(2,4-Dihydroxy-5-isopropylbenzoyl)isoindolin-5-yl)methyl)piperazin-1-yl)-8-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)octane-1,8-dione

参考文献

1. Wei Liu, et al. J Med Chem. 2025 Oct 9;68(19):19933-19954.

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