| Bioactivity | Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice[1]. |
| Invitro | Topoisomerase I inhibitor 17 (5-500 nM, 72 h) 对四种癌细胞 (HepG2、A549、HeLa 和 HCT116) 抗增殖，其 IC50 分别为 136.6, 33.7, 72.9 和 36.1 nM[1]。Topoisomerase I inhibitor 17 可穿过 Caco-2 细胞单层，从顶端到基底侧的表观渗透系数为 2.24 μcm/s (0.5-1.0 μM, 4 h)，Caco-2 细胞的存活率超过 90% (0.2-1.0 μM, 4 h)[1]。Topoisomerase I inhibitor 17 (5-100 nM, 12-72 h) 显著抑制增殖诱导的集落形成，浓度依赖性抑制 HCT116 细胞迁移，增加 ROS 生成[1]。Topoisomerase I inhibitor 17 (0-50 μM, 48 h) 以剂量依赖性方式诱导 HCT116 细胞凋亡和细胞周期停滞，阻止 G2/M 检查点的进展[1]。Topoisomerase I inhibitor 17 抑制 HCT116 细胞中的 DDX5 表达 (100 μM, 48-72 h)，解除 DDX5 阻断的 Top1 活性 (5 和 50 μM)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Topoisomerase I inhibitor 17 相关抗体: Cell Cycle Analysis[1] Cell Line: |
| In Vivo | Topoisomerase I inhibitor 17 (2-15 mg/kg, i.p., 一周一次，持续 4 周) 通过浓度依赖性的肿瘤抑制作用和可接受的毒性，有效减少人结肠癌 PDX 肿瘤小鼠的肿瘤[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 2413582-45-1 |
| Formula | C28H21FN2O7 |
| Molar Mass | 516.47 |
| 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]. Wang, et al. Design, synthesis and investigation of biological activity and mechanism of fluoroaryl-substituted derivatives at the FL118 position 7. European journal of medicinal chemistry. 2024, 283, 117143. |
Topoisomerase I inhibitor 17
CAS: 2413582-45-1 F: C28H21FN2O7 W: 516.47
Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces D
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.