Vinflunine ditartrate(Synonyms: 酒石酸长春氟宁)

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Vinflunine ditartrate (Synonyms: 酒石酸长春氟宁)

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。

Vinflunine ditartrate(Synonyms: 酒石酸长春氟宁)

Vinflunine ditartrate Chemical Structure

CAS No. : 194468-36-5

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生物活性

Vinflunine ditartrate is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine ditartrate has anti-angiogenic, vascular-disrupting and anti-metastatic activities. Vinflunine ditartrate can be used for the research of transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and carcinoma of the breast[1][2].

IC50 & Target

microtubule[1]

体外研究
(In Vitro)

Vinflunine (0.01-10 μM; 45 min) induces a rapid change in endothelial cell shape: cells retracted and assumed a rounded morphology[2].
Vinflunine (0.01-10 μM; 1 h) disrupts newly formed capillary-like structures[2].
Vinflunine (0.01-10 μM; 1 h) inhibits endothelial cell motility, with an IC50 of 0.71 μM[2].
Vinflunine (0.001-10 μM; 1-72 h) inhibits endothelial cell proliferation in vitro[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Vinflunine (0.08-20 mg/kg; i.v.) reduces the number of experimental liver metastases by human LS174T colon cancer cells[2].
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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (BALB/c/Ola/Hsd-nu) were implanted LS174T cells[2]
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.

Clinical Trial

分子量

1117.10

Formula

C53H66F2N4O20

CAS 号

194468-36-5

中文名称

酒石酸长春氟宁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • [1]. Bennouna J, et, al. Vinflunine: a new microtubule inhibitor agent. Clin Cancer Res. 2008 Mar 15;14(6):1625-32.

    [2]. Kruczynski A, et, al. Anti-angiogenic, vascular-disrupting and anti-metastatic activities of vinflunine, the latest vinca alkaloid in clinical development. Eur J Cancer. 2006 Nov;42(16):2821-32.

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