Indibulin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Indibulin 是一种合成小分子，具有抗有丝分裂和潜在的抗肿瘤活性。Indibulin 是一种口服微管蛋白组装抑制剂，显示出有效的抗癌活性，且神经毒性最小。

Indibulin is a synthetic small molecule with antimitotic and potential antineoplastic activities.Indibulin ?an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity.?Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.Indibulin, a synthetic inhibitor of tubulin assembly, has shown promising anticancer activity.?Using time-lapse confocal microscopy, indibulin dampens the dynamic instability of individual microtubules in live breast cancer cells.?Indibulin treatment also perturbed the localization of end-binding proteins at the growing microtubule ends in MCF-7 cells.?Indibulin reduced inter-kinetochoric tension, produced aberrant spindles, activated mitotic checkpoint proteins Mad2 and BubR1, and induced mitotic arrest in MCF-7 cells.?Indibulin-treated MCF-7 cells underwent apoptosis-mediated cell death.?Further, the combination of indibulin with an anticancer drug vinblastine was found to exert synergistic cytotoxic effects on MCF-7 cells.?Interestingly, indibulin displayed a stronger effect on the undifferentiated neuroblastoma (SH-SY5Y) cells than the differentiated neuronal cells.?Unlike indibulin, vinblastine and colchicine produced similar depolymerizing effects on microtubules in both differentiated and undifferentiated SH-SY5Y cells.(In Vitro):Indibulin (300-2100 nM; 48?hours) inhibits the proliferation of MCF-7 cells with an IC50 of 150?nM.Indibulin (300, 600 nM; 48?hours) blockes the cells in the G2/M phase indicating that indibulin blockes the progression of the cell cycle at mitosis.Indibulin (150-600 nM; 24?hours) induces apoptosis in MCF-7 cells.Indibulin (150-600 nM; 48?hours) with 300 and 600?nM generates cleaved fragments of PARP protein the treatment of MCF-7 cells.

Indibulin (300-2100 nM; 48?hours) inhibits the proliferation of MCF-7 cells with an IC50 of 150?nM. Indibulin (300, 600 nM; 48?hours) blockes the cells in the G2/M phase indicating that indibulin blockes the progression of the cell cycle at mitosis. Indibulin (150-600 nM; 24?hours) induces apoptosis in MCF-7 cells. Indibulin (150-600 nM; 48?hours) with 300 and 600?nM generates cleaved fragments of PARP protein the treatment of MCF-7 cells. Cell Proliferation Assay Cell Line:MCF-7 cells Concentration:300, 600, 900, 1200, 1500, 1800, 2100 nM Incubation Time:48?hours Result:Inhibited the proliferation of MCF-7 cells with an IC50 of 150?nM.Cell Cycle Analysis Cell Line:MCF-7 cells Concentration:300, 600 nM Incubation Time:48?hours Result:Blocked the cells in the G2/M phase of the cell cycle. Apoptosis AnalysisCell Line:MCF-7 cells Concentration:150, 300 and 600?nM Incubation Time:24?hours Result:Induced apoptosis in MCF-7 cells.Western Blot Analysis Cell Line:MCF-7 cells Concentration:150, 300 and 600?nM Incubation Time:48?hours Result:Generated cleaved fragments of PARP protein in 300 and 600?nM.

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ZIO 301,D 24851

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Tubulin

cancer

Metastatic Breast Cancer

204205-90-3

389.83

C22H16ClN3O2

>98% (HPLC)

DMSO:50 mg/mL (128.26 mM; Need ultrasonic)

O=C(NC1=CC=NC=C1)C(C2=CN(CC3=CC=C(Cl)C=C3)C4=C2C=CC=C4)=O

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(-20℃)

With Ice Pack

≥ 2 years