1. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  2. Topoisomerase HDAC Reactive Oxygen Species Apoptosis
  3. Top/HDAC-IN-3

Top/HDAC-IN-3 (Compound 31) 是一种具有口服活性的 TopoisomeraseHDAC 的双重抑制剂。Top/HDAC-IN-3 通过增加活性氧 (ROS) 水平,导致 DNA 损伤,从而 抑制癌细胞的克隆形成和迁移, 诱导癌细胞凋亡 (Apoptosis) 和细胞周期阻滞。Top/HDAC-IN-3 在 NSCLC 模型中展现出显著的抗肿瘤作用,抗肿瘤效率 (TGI = 77.5%,100 mg/kg) 优于 HDAC 抑制剂 SAHA (HY-10221) 以及 SAHA (HY-10221) 与拓扑异构酶抑制剂伊立替康 (HY-16562) 的联合处理效果。

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Top/HDAC-IN-3 Chemical Structure

Top/HDAC-IN-3 Chemical Structure

CAS No. : 3059615-90-3

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  • 生物活性

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生物活性

Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562)[1].

分子量

435.47

Formula

C24H25N3O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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产品名称:
Top/HDAC-IN-3
目录号:
HY-159966
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