Topo I-IN-1

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Topo I-IN-1 

Topo I-IN-1 (Compound 14d) 是一种具有抗肿瘤活性和DNA嵌入能力的 Topo I抑制剂。Topo I-IN-1 诱导细胞凋亡 (apoptosis)。

Topo I-IN-1

Topo I-IN-1 Chemical Structure

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生物活性

Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor with antitumor activity and DNA intercalative capability. Topo I-IN-1 induces cell apoptosis[1].

IC50 & Target

Topoisomerase I

 

体外研究
(In Vitro)

Topo I-IN-1 (Compound 14d) (0-50 µM, 48 h) shows antiproliferative activity against human cancer cells and has low toxicity toward normal rat kidney epithelial cells[1].
Topo I-IN-1 (0-4 µM, 48 h) shows a dose-dependent apoptotic effect, induces ROS generation, and inhibits cell migration[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: A549, HCT116, MCF7, SK-MEL-28, and NRK (normal rat kidney epithelial cells)
Concentration: 0-50 µM
Incubation Time: 48 h
Result: Showed in vitro cytotoxicity with IC50 values of 2.33 ± 1.52, 2.85 ± 0.83, 26.23 ± 2.48, 3.86 ± 0.33, and 29.99 ± 0.95 µM against A549, HCT116, MCF7, SK-MEL-28, and NRK cells, respectively.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 2, 2.33 and 4 μM
Incubation Time: 48 h
Result: Resulted in the morphological changes typical to apoptosis.

分子量

408.25

Formula

C20H14BrN3O2
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.
参考文献

  • [1]. Manasa Kadagathur, et al. Synthesis of indolo/pyrroloazepinone-oxindoles as potential cytotoxic, DNA-intercalating and Topo I inhibitors. Bioorg Chem. 2022 May;122:105706.

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