1. Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. A-259745

A-259745 是一种具有口服活性的抗有丝分裂剂,结合到微管蛋白 (tubulin) 的秋水仙碱结合位点。A-259745 对多药耐药和非多药耐药癌细胞系均表现出强效的体外细胞毒活性,对 HCT-15 和 NCI-H460 细胞系的 ED50 值分别为 0.018 μM 和 0.028 μM。A-259745 抑制微管蛋白 (tubulin) 聚合作用,破坏有丝分裂纺锤体的动态平衡,使分裂细胞停滞在中后期,并随后诱导凋亡 (apoptosis)。A-259745 在小鼠肿瘤模型中显示出剂量依赖性的抗肿瘤疗效。A-259745 可用于癌症研究。

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A-259745

A-259745 Chemical Structure

CAS No. : 256934-83-5

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生物活性

A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer[1].

分子量

366.41

Formula

C21H22N2O4

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.

纯度 & 产品资料
参考文献
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
A-259745
目录号:
HY-101741
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