Indibulin是一种口服有效的微管蛋白合成抑制剂，具有抗有丝分裂和抗肿瘤活性，且神经毒性小。它降低了肌间神经张力，产生异常的纺锤体，激活有丝分裂检查点蛋白 Mad2 和 BubR1，并诱导有丝分裂停滞和细胞凋亡。

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.

204205-90-3

C22H16ClN3O2

389.83

ZIO 301;D 24851;2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺

DMSO:50 mg/mL (128.26 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years