产品说明书

Vinorelbine

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Chemical Structure| 71486-22-1 同义名 : -
CAS号 : 71486-22-1
货号 : A970401
分子式 : C45H54N4O8
纯度 : 98%
分子量 : 778.93
MDL号 : MFCD00866248
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM[3]. Vinorelbine time-dependently induces the p53 and p21 WAFI/CIP1 expression in androgen-dependent (AD) and- independent (AI) prostate cancer cell lines. Vinorelbine stimulates reporter genes in a concentration-dependent manner. Exposure of AI cells to paciltaxel followed by vinorelbine produced synergism[4]. The combination of vinorelbine with nontoxic concentrations of ME0328 (PARP3 inhibitor) or olaparib reduces vinorelbine resistance by 10 and 17 fold, respectively, potentiating vinorelbine-induced arrest at the G2/M boundary[5]. Vinorelbine is tolerated at a weekly interval in tumor-bearing cats, with an MTD (maximal tolerated dose) of 11.5 mg/m2[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03117335 Advanced Non-small Cell Lung C... 展开 >>ancer 收起 << Phase 3 Completed - -
NCT00432562 Breast Cancer ... 展开 >> Non-small Cell Lung Cancer Non-Hodgkins Lymphoma 收起 << Phase 1 Completed - Argentina ... 展开 >> Clinical Investigative Site Buenos Aires, Argentina Clinical Investigative Site Mendoza, Argentina Clinical Investigative Site Rosario, Argentina Clinical Investigative Site Santa Fe, Argentina Clinical Investigative Site Tucuman, Argentina 收起 <<
NCT00602797 Recurrent Non-Small Cell Lung ... 展开 >>Carcinoma Stage IV Non-Small Cell Lung Cancer 收起 << Phase 2 Completed - United States, Nebraska ... 展开 >> CHI Health Saint Francis Grand Island, Nebraska, United States, 68803 Great Plains Regional Medical Center North Platte, Nebraska, United States, 69103 Omaha Veterans Administration Medical Center Omaha, Nebraska, United States, 68105 University of Nebraska Medical Center Omaha, Nebraska, United States, 68198 United States, South Dakota Avera McKennan Hospital and University Health Center Sioux Falls, South Dakota, United States, 57105 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.28mL

0.26mL

0.13mL

6.42mL

1.28mL

0.64mL

12.84mL

2.57mL

1.28mL
参考文献

[1]Poirier VJ, Burgess KE, Adams WM, Vail DM. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.

[2]Photiou A, Sheikh MN, Bafaloukos D, Retsas S. Antiproliferative activity of vinorelbine (Navelbine) against six human melanoma cell lines. J Cancer Res Clin Oncol. 1992;118(4):249-54.

[3]Ngan VK, Bellman K, Hill BT, Wilson L, Jordan MA. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001;60(1):225-232

[4]Liu XM, Jiang JD, Ferrari AC, Budman DR, Wang LG. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003;89(8):1566-1573

[5]Sharif-Askari B, Amrein L, Aloyz R, Panasci L. PARP3 inhibitors ME0328 and olaparib potentiate vinorelbine sensitization in breast cancer cell lines. Breast Cancer Res Treat. 2018;172(1):23-32

[6]Pierro JA, Mallett CL, Saba CF. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013;27(4):943-948