酒石酸长春氟宁 | 194468-36-5

• 分子结构分类: 有机化合物 - 生物碱及其衍生物
• 中文名称: 酒石酸长春氟宁
• 中文别名: D-葡萄糖醇,6-氨基-2,5-脱水-1,6-二脱氧-(9CI)
• 英文名称: Vinflunine (Tartrate)
• 英文别名: (2R,3R)-2,3-dihydroxybutanedioic acid;methyl (1R,9R,10S,11R,12R,19R)-11-acetyloxy-4-[(12S,14S,16R)-16-(1,1-difluoroethyl)-12-methoxycarbonyl-1,10-diazatetracyclo[12.3.1.03,11.04,9]octadeca-3(11),4,6,8-tetraen-12-yl]-12-ethyl-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carboxylate
• CAS: 194468-36-5
• 化学式: C49H60F2N4O14
• 分子量: 967.0
• InChiKey: TXONSEMUKVZUON-MSNAZLETSA-N

物化性质

• 熔点：
  244-246°C (dec)
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  2.96
• 重原子数：
  69
• 可旋转键数：
  13
• 环数：
  9.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  249
• 氢给体数：
  6
• 氢受体数：
  19

制备方法与用途

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.