|2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺|CsnPharm

CAS No.: 204205-90-3

2-(1-(4-Chlorobenzyl)-1H-indol-3-yl)-2-oxo-N-(pyridin-4-yl)acetamide Catalog No. CSN23867

Synonyms: ZIO 301;D 24851;ZIO-301；ZERO/005632；ZINC01996564；d-24851

Indibulin is a microtubule destabilizer that blocks tubulin polymerization with IC50 of 0.3 μM.

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技术信息

生物活性

描述Microtubules are dynamic polymers involved in a multitude of cellular processes. Indibulin is a small-molecule microtubule inhibitor that exhibits antitumor activity but does not cause neurotoxicity. Indibulin dose-dependently inhibited the polymerization of purified calf brain tubulin with an IC50 value of ~0.25μM and a maximal inhibition of 90%. ^[1] Indibulin inhibited the proliferation of MCF-7 cells with an IC50 value of 150 ± 13nM. Cells treated with 600nM indibulin showed an increased percentage of phosphohistone H3 (S10) compared to the control group. The disruption of the microtubule network was observed when MCF-7 cells were treated with 300nM indibulin. In cells incubated with 600nM indibulin, most of the microtubules were depolymerized compared to the control group. The rates of growth and shortening states of microtubules in MCF-7 cells were reduced by 37 and 53%, respectively, in the presence of 150nM indibulin. Treatment of MCF-7 cells with indibulin (300 and 600nM) increased the levels of Mad2 and BubR1 and activated apoptotic cell death. The combination of indibulin (50 and 150nM) and 1nM vinblastine inhibited the proliferation of MCF-7 cells by 53 and 71%, respectively.^[2] In a rat Yoshida AH13 sarcoma model, administration of indibulin (10mg/kg, p.o.) for two weeks resulted in complete tumor remissions.^[3]
作用机制Indibulin is a synthetic inhibitor of tubulin assembly that inhibits microtubule dynamics by blocking mitosis.^[2]
参考文献

[1] Wienecke A, Bacher G. Indibulin, a novel microtubule inhibitor, discriminates between mature neuronal and nonneuronal tubulin. Cancer Res. 2009;69(1):171-177. doi:10.1158/0008-5472.CAN-08-1342
[2] Kapoor S, Srivastava S, Panda D. Indibulin dampens microtubule dynamics and produces synergistic antiproliferative effect with vinblastine in MCF-7 cells: Implications in cancer chemotherapy. Sci Rep. 2018;8(1):12363. Published 2018 Aug 17. doi:10.1038/s41598-018-30376-y
[3] Bacher G, Nickel B, Emig P, et al. D-24851, a novel synthetic microtubule inhibitor, exerts curative antitumoral activity in vivo, shows efficacy toward multidrug-resistant tumor cells, and lacks neurotoxicity. Cancer Res. 2001;61(1):392-399.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5652 mL
- 12.8260 mL
- 25.6519 mL
- 5 mM
- 0.5130 mL
- 2.5652 mL
- 5.1304 mL
- 10 mM
- 0.2565 mL
- 1.2826 mL
- 2.5652 mL

技术信息

CAS号

204205-90-3

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H16ClN3O2

运输

蓝冰

分子量

389.83

别名

ZIO 301;D 24851;ZIO-301；ZERO/005632；ZINC01996564；d-24851;D-24851；NCGC00160428-01

溶解度

DMSO	40.0 mg/mL (102.6 mM)
Water	Insoluble
Ethanol	Insoluble

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2-(1-(4-Chlorobenzyl)-1H-indol-3-yl)-2-oxo-N-(pyridin-4-yl)acetamide Catalog No. CSN23867

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