| Hazard Information | Back Directory | [Uses]
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4%[1]. | [in vivo]
TOPOI/PARP-1-IN-1 (40 mg/kg; p.o.; once every two days, for a total of 17 days) inhibits HGC-27 tumor growth in xenograft tumor mice model[1]. | Animal Model: | Female BALB/c nude mice (xenograft tumor model of HGC-2 cells)[1]. | | Dosage: | 40 mg/kg | | Administration: | Oral administration; once every two days, for a total of 17 days | | Result: | Exhibited tumor growth inhibition rate (TGI) of 75.4% in mice. |
| [References]
[1] Qiu G, et al. Design, synthesis and biological evaluation of matrine contains benzimidazole derivatives as dual TOPOI and PARP inhibitors for cancer therapy. Eur J Med Chem. 2024 Mar 27;270:116348. DOI:10.1016/j.ejmech.2024.116348 |
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