194468-36-5
中文名称
酒石酸长春氟宁
英文名称
Vinflunine Ditartrate
CAS
194468-36-5
分子式
C49H59F2N4O14
分子量
966.008
MOL 文件
194468-36-5.mol
更新日期
2023/03/20 15:41:19
194468-36-5 结构式
基本信息
英文别名
JavlorF 12158
BMS 710485
Ditartrate
Vinflunine Ditartrate
20',20'-Difluoro-3',4'-dihydrovinorelbine Ditartrate
4'-Deoxy-20',20'-difluoro-5'-norvincaleukoblastine Ditartrate
(2β,3β,4β,5α,12β,19α)-4-(Acetyloxy)-6,7-didehydro-15-[(2R,4R,6S,8S)-4-(1,1-difluoroethyl)-1,3,4,5,6,7,8,9-octahydro-8-(Methoxycarbonyl)-2,6-Methano-2H-azecino[4,3-b]indol-8-yl]-3-hydroxy-16-Methoxy-1-MethylaspidosperMidine-3-carboxylic Acid Methyl Ester (2R,3R)-2,3-Dihydroxybutanedioate
物理化学性质
熔点244-246°C (dec)
储存条件-20°C冷冻
溶解度DMSO (Slightly), Methanol (Slightly)
形态Solid
颜色White to Light Beige
常见问题列表
生物活性
Vinflunine ditartrate 是一种长春花生物碱家族的氟化微管抑制剂。Vinflunine ditartrate 具有抗血管生成，破坏血管和抗转移的活性。Vinflunine ditartrate 可用于尿路上皮移行细胞癌，非小细胞肺癌和乳腺癌的研究。靶点
microtubule
体外研究
Vinflunine (0.01-10 μM; 45 min) induces a rapid change in endothelial cell shape: cells retracted and assumed a rounded morphology.
Vinflunine (0.01-10 μM; 1 h) disrupts newly formed capillary-like structures.
Vinflunine (0.01-10 μM; 1 h) inhibits endothelial cell motility, with an IC
50
of 0.71 μM.
Vinflunine (0.001-10 μM; 1-72 h) inhibits endothelial cell proliferation in vitro.
体内研究
Vinflunine (0.08-20 mg/kg; i.v.) reduces the number of experimental liver metastases by human LS174T colon cancer cells.
Vinflunine (0.63-5 mg/kg; i.v. before and 2 d after Matrigel implantation) inhibits the bFGF-induced angiogenic response in mice in a dose-dependent manner.
| Animal Model: | Female athymic nude mice (BALB/c/Ola/Hsd-nu) were implanted LS174T cells |
| Dosage: | 0.08, 0.16, 1.25, 5, 10, 20 mg/kg |
| Administration: | I.v. on days 4, 7, 11, 14, 18 and 21 after tumour cell implantation |
| Result: | Induced a dose-dependent reduction in the number of metastatic foci at the surface of the liver and was well tolerated. |