Indibulin (ZIO 301)，一种口服有效的微管蛋白合成抑制剂，具有良好的抗癌活和极小的神经毒性。Indibulin 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。
CAS：204205-90-3
分子式：C22H16ClN3O2
分子量：389.83
纯度：98%
存储：Store at -20°C

Background:

Indibulin (ZIO 301) , 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[1]. Tubulin[1]

Indibulin (300-2100 nM; 48 hours) inhibits the proliferation of MCF-7 cells with an IC50 of 150 nM[1]. 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[1]. Indibulin (150-600 nM; 24 hours) induces apoptosis in MCF-7 cells[1]. Indibulin (150-600 nM; 48 hours) with 300 and 600 nM generates cleaved fragments of PARP protein the treatment of MCF-7 cells[1]. Cell Proliferation Assay[1] Cell Line: MCF-7 cells

[1]. Kapoor S, et al. Indibulin dampens microtubule dynamics and produces synergistic antiproliferative effect with vinblastine in MCF-7 cells: Implications in cancer chemotherapy. Sci Rep. 2018 Aug 17;8(1):12363.