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ARN24139 Sale

目录号 : GC46880

A topoisomerase II poison

ARN24139 Chemical Structure

Cas No.:2699768-78-8

规格 价格 库存 购买数量
1 mg
¥942.00
现货
5 mg
¥4,009.00
现货
10 mg
¥7,538.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

ARN24139 is a topoisomerase II poison (IC50 = 7.3 µM in a topoisomerase II decatenation assay).1 It inhibits proliferation of DU145, HeLa, and A549 cells (IC50s = 4.7, 3.8, and 3.1 µM, respectively).

1.Arencibia, J.M., Brindani, N., Franco-Ulloa, S., et al.Design, synthesis, dynamic docking, biochemical characterization, and in vivo pharmacokinetics studies of novel topoisomerase II poisons with promising antiproliferative activityJ. Med. Chem.63(7)3508-3521(2020)

Chemical Properties

Cas No. 2699768-78-8 SDF
Canonical SMILES S=C(N1C2=CC=CC=C2)N(C3=CC=CC=C3)C(O)=C(C(NC4=CC(OC(F)(F)F)=CC=C4)=O)C1=O
分子式 C24H16F3N3O4S 分子量 499.5
溶解度 DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 10 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.002 mL 10.01 mL 20.02 mL
5 mM 0.4004 mL 2.002 mL 4.004 mL
10 mM 0.2002 mL 1.001 mL 2.002 mL
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Research Update

Design, Synthesis, Dynamic Docking, Biochemical Characterization, and in Vivo Pharmacokinetics Studies of Novel Topoisomerase II Poisons with Promising Antiproliferative Activity

J Med Chem 2020 Apr 9;63(7):3508-3521.PMID:32196342DOI:PMC7997578

We previously reported a first set of hybrid topoisomerase II (topoII) poisons whose chemical core merges key pharmacophoric elements of etoposide and merbarone, which are two well-known topoII blockers. Here, we report on the expansion of this hybrid molecular scaffold and present 16 more hybrid derivatives that have been designed, synthesized, and characterized for their ability to block topoII and for their overall drug-like profile. Some of these compounds act as topoII poison and exhibit good solubility, metabolic (microsomal) stability, and promising cytotoxicity in three cancer cell lines (DU145, HeLa, A549). Compound 3f (ARN24139) is the most promising drug-like candidate, with a good pharmacokinetics profile in vivo. Our results indicate that this hybrid new chemical class of topoII poisons deserves further exploration and that 3f is a favorable lead candidate as a topoII poison, meriting future studies to test its efficacy in in vivo tumor models.