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DDO3602

Catalog No.GC81720 Copy One-Click Copy Product Info

DDO3602 is a PARP1 HSPTAC ( HSP90 -mediated proteolysis-targeting chimera) degrader, with a DC50 of 490.3 nM against PARP1; its K d values for PARP1 and HSP90 are 66.5 nM and 1.64 nM, respectively.

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DDO3602 Chemical Structure

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5mg
$1,557.00
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Sample solution is provided at 25 µL, 10mM.



Description of DDO3602

DDO3602 is a PARP1 HSPTAC ( HSP90 -mediated proteolysis-targeting chimera) degrader, with a DC50 of 490.3 nM against PARP1; its K d values for PARP1 and HSP90 are 66.5 nM and 1.64 nM, respectively. DDO3602 induces the formation of an unnatural PARP1-HSP90 ternary complex, recruits E3 ubiquitin ligase, and promotes PARP1 degradation via the ubiquitin-proteasome pathway. DDO3602 induces G2/M cell cycle arrest, DNA damage, inhibits cell migration, and exhibits antiproliferative activity in breast cancer cells. DDO3602 can be used in breast cancer-related research [1]. (Pink: PARP1 ligand; Blue: HSP90 ligand; Black: linker ).

In Vivo, DDO3602 (10-20 mg/kg; i.p.; every other day; 21 days) potently inhibits MCF-7 xenograft tumor growth in immunocompromised mice[1]. DDO3602 (20 mg/kg; i.v.; single dose) exhibits tumor-targeted pharmacokinetics in MCF-7 xenograft mice, with significantly higher accumulation in tumor tissue than normal tissues following a single 20 mg/kg intravenous dose[1].

In Vitro, DDO3602 (0-3 μM; 9 h) degrades PARP1 in human breast cancer MCF-7 cells in a dose-dependent manner, with a DC50 of 490.3 nM, and the degradation rate reaches 70.6% after incubation at 1 μM for 9 h[1]. DDO3602 (1 μM; 0-24 h) induces significant degradation of PARP1 in human breast cancer MCF-7 cells within 3 h, with nearly complete depletion achieved by 9 h[1]. DDO3602 (1 μM; 0-24 h) degrades the pre-existing PARP1 protein in MCF-7 human breast cancer cells, rather than inhibiting its synthesis[1]. DDO3602 (0-1 μM) exerts a stronger inhibitory effect on colony formation in human breast cancer MCF-7 cells than in normal mammary epithelial MCF-10A cells[1]. DDO3602 (0-10 μM; 72 h) inhibits the viability of MCF-7 human breast cancer cells with an IC50 of 0.189 μM; its potency is approximately 4-fold higher than that against MCF-10A normal mammary epithelial cells (IC50 = 0.744 μM) after 72 h of treatment[1]. DDO3602 (0.5-1 μM; 24 h) induces dose-dependent G2/M cell cycle arrest in human breast cancer MCF-7 cells[1]. DDO3602 (1 μM; 24 h) induces significant DNA double-strand break formation in MCF-7 human breast cancer cells (detected by γ-H2A.X accumulation)[1]. DDO3602 (0.1-1 μM; 48 h) significantly inhibits the migration of MCF-7 cells[1].

References:
[1]. Liu W, et al. HSP90 Mediates Targeted Degradation of Nonclient Protein PARP1 for Breast Cancer Treatment. Journal of medicinal chemistry. 2025 Oct 09;68(19):19933-19954.

Chemical Properties of DDO3602

Cas No. SDF
Formula C51H58FN7O7 M.Wt 900.05
Solubility Storage Store at -20°C
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of DDO3602

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1 mg 5 mg 10 mg
1 mM 1.111 mL 5.5552 mL 11.1105 mL
5 mM 222.2 μL 1.111 mL 2.2221 mL
10 mM 111.1 μL 555.5 μL 1.111 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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