| Bioactivity | 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 was 75.4%[1]. |
| Target | IC50: 0.09 μM (PARP1). |
| Invitro | TOPOI/PARP-1-IN-1 (1.25-5 μM; 48 h) 以浓度依赖的方式抑制 HGC-27 细胞的增殖和迁移[1]。TOPOI/PARP-1-IN-1 (1.25-5 μM; 24 h) 以剂量依赖的方式诱导 HGC-27 细胞凋亡[1]。TOPOI/PARP-1-IN-1 在 HGC-27 细胞中诱导 DNA 损伤，并抑制 TOPOI 蛋白的表达[1]。TOPOI/PARP-1-IN-1 具有抗肿瘤活性，对 HeLa、A549、HepG-2 和 HGC-27 细胞的 IC50 值分别为 7.21 μM、9.48 μM、3.80 μM 和 2.49 μM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> TOPOI/PARP-1-IN-1 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| In Vivo | TOPOI/PARP-1-IN-1 (40 mg/kg; p.o.; once every two days, for a total of 17 days) 抑制异种移植小鼠模型中的 HGC-27 肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 2948352-16-5 |
| Formula | C36H38Br2N4O2 |
| Molar Mass | 718.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
TOPOI/PARP-1-IN-1
CAS: 2948352-16-5 F: C36H38Br2N4O2 W: 718.52
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09
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