Cevipabulin

微管聚合的激活剂；诱导分离的牛脑微管蛋白聚集；在无细胞测定中，浓度为100µM时抑制长春花碱与微管蛋白的结合；浓度为68nM时诱导HeLa细胞有丝分裂阻滞；对各种癌细胞系有细胞毒性(IC50s=18-40nM)；静脉注射20mg/kg时，可降低LoVo结肠腺癌小鼠异种移植模型中的肿瘤生长。An activator of microtubule polymerization; induces aggregation of isolated bovine brain tubulin; inhibits binding of vinblastine to tubulin in cell-free assays at 100 µM; induces mitotic block in HeLa cells when used at a concentration of 68 nM; cytotoxic to various cancer cell lines (IC50s = 18-40 nM); reduces tumor growth in a LoVo colon adenocarcinoma mouse xenograft model at 20 mg/kg, i.v.分子式C18H18ClF5N6O分子量464.8FC(F)(F)[C@H](C)NC1=C(C2=C(C=C(C=C2F)OCCCNC)F)C(Cl)=NC3=NC=NN31