产品
编 号:F478601
分子式:C18H18ClF5N6O
分子量:464.82
产品类型
结构图
CAS No: 849550-05-6
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产品详情
生物活性:
Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
体内研究:
Cevipabulin (TTI-2370)( 5, 10, 15, and 20 mg/kg, every 4 days for 4 cycles, in mice) is active by i.v. and p.o. administration against human tumor xenografts, showing dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg.Animal Model:Athymic nu/nu female mice implanted s.c. in the flank with 1×107 LoVo human colon adenocarcinoma cells
Dosage:5, 10, 15, and 20 mg/kg
Administration:I.V. injection every 4 days for 4 cycles.
Result:The compound showed dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg.
Animal Model:Athymic nu/nu female mice implanted s.c. in the flank with 1×106 U87-MG human glioblastoma cells.
Dosage:25 mg/kg
Administration:P.O. or I.V.
Result:The compound was active by p.o. or i.v. administration against human tumor xenografts.
体外研究:
Cevipabulin (0-50 nM, 72 hours) shows good activity (between 18 and 40 nM IC50 values) on cell lines from ovarian, breast, prostate, and cervical tumors.Flow cytometry experiments reveal that, Cevipabulin (TTI-237) at low concentrations (20-40 nM) produces sub-G1 nuclei and, at concentrations above 50 nM, it causes a strong G2-M block.