Vinorelbine ditartrate
(Synonyms: 酒石酸长春瑞滨; KW-2307; Nor-5'-anhydrovinblastine ditartrate) 目录号 : GC14806
Vinorelbine ditartrate是一种抗有丝分裂药物，是紫杉醇（Paclitaxel）的一种半合成衍生物，通过抑制肿瘤细胞的微管聚合来发挥抗肿瘤作用，主要用于治疗非小细胞肺癌和转移性乳腺癌等恶性肿瘤。
Cas No.:125317-39-7
Sample solution is provided at 25 µL, 10mM.
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Vinorelbine ditartrate is an anti-mitotic drug, a semi-synthetic derivative of paclitaxel, that exerts its antitumor effect by inhibiting microtubule polymerization in tumor cells. Vinorelbine ditartrate is primarily used to treat malignant tumors such as non-small cell lung cancer and metastatic breast cancer[1, 2]. Vinorelbine ditartrate rapidly and reversibly binds to soluble tubulin, inducing conformational changes, enhancing the affinity of microtubules themselves, significantly reducing the rate of microtubule dynamics (elongation and shortening), and prolonging the duration of microtubules in the attenuated state[3]. Vinorelbine ditartrate can induce p53 and p21WAFI/CIP1 expression in androgen-dependent (AD) and androgen-independent (AI) prostate cancer cell lines[4]. Vinorelbine ditartrate can hinder the timely progression of meiosis maturation in mice and induce aneuploidy in mouse oocytes[5].
In vitro, Vinorelbine ditartrate (0.1-36nM) treatment of HOS and MG-63 osteosarcoma cells for 8-72h inhibited the growth of both cell lines in a dose- and time-dependent manner and induced apoptosis[6]. Vinorelbine ditartrate (0.5-6nM) treatment of human breast cancer cell lines (MCF 7, ZR 75-1, and T 47-D cells) for 24h inhibited the growth of the three cell lines in a dose-dependent manner and induced apoptosis[7].
In vivo, Vinorelbine ditartrate (30mg/kg) administered intravenously to mice xenografted with 3LL lung cancer cells almost completely inhibited tumor growth and the production of malignant pleural effusion (MPE), significantly reducing tumor angiogenesis and vascular endothelial growth factor (VEGF) expression[8].
References:
[1] Kumar B, Kumar R, Skvortsova I, et al. Mechanisms of tubulin binding ligands to target cancer cells: updates on their therapeutic potential and clinical trials[J]. Current cancer drug targets, 2017, 17(4): 357-375.
[2] Ngan V K, Bellman K, Hill B T, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids Vinorelbine ditartrate and its newer derivative vinflunine[J]. Molecular pharmacology, 2001, 60(1): 225-232.
[3] Capasso A. Vinorelbine ditartrate in cancer therapy[J]. Current drug targets, 2012, 13(8): 1065-1071.
[4] Liu X M, Jiang J D, Ferrari A C, et al. Unique induction of p21WAF1/CIP1expression by Vinorelbine ditartrate in androgen-independent prostate cancer cells[J]. British journal of cancer, 2003, 89(8): 1566-1573.
[5] Cheng S Y, Yi Z Y, Zhang C H, et al. Vinorelbine ditartrate administration impedes the timely progression of meiotic maturation and induces aneuploidy in mouse oocytes[J]. Reproductive Toxicology, 2024, 128: 108634.
[6] Roncuzzi L, Marti G, Baiocchi D, et al. Effect of Vinorelbine ditartrate on cell growth and apoptosis induction in human osteosarcoma in vitro[J]. Oncology reports, 2006, 15(1): 73-77.
[7] Weigel M T, Meinhold-Heerlein I, Bauerschlag D O, et al. Combination of imatinib and Vinorelbine ditartrate enhances cell growth inhibition in breast cancer cells via PDGFR β signalling[J]. Cancer letters, 2009, 273(1): 70-79.
[8] Cui R, Yoshioka M, Takahashi F, et al. Vinorelbine ditartrate is effective for the malignant pleural effusion associated with lung cancer in mice[J]. Anticancer research, 2008, 28(3A): 1633-1639.
Vinorelbine ditartrate是一种抗有丝分裂药物，是紫杉醇（Paclitaxel）的一种半合成衍生物，通过抑制肿瘤细胞的微管聚合来发挥抗肿瘤作用，主要用于治疗非小细胞肺癌和转移性乳腺癌等恶性肿瘤[1, 2]。Vinorelbine ditartrate能够与可溶性微管蛋白的快速且可逆结合，诱导构象变化，增强微管自身的亲和力，显著降低了微管动态的速率（延长和缩短），并延长了微管在衰减状态下的持续时间[3]。Vinorelbine ditartrate能够在雄激素依赖性（AD）和非依赖性（AI）前列腺癌细胞系中，诱导p53和p21WAFI/CIP1表达[4]。Vinorelbine ditartrate能够阻碍小鼠减数分裂成熟的及时进展，并诱导小鼠卵母细胞出现非整倍体[5]。
在体外，Vinorelbine ditartrate（0.1-36nM）处理HOS和MG-63骨肉瘤细胞8-72h，以剂量和时间依赖性方式抑制了两种细胞系的生长，诱导了细胞凋亡[6]。Vinorelbine ditartrate（0.5-6nM）处理人类乳腺癌细胞系（MCF 7、ZR 75-1和T 47-D细胞）24h，以剂量依赖性方式抑制了三种细胞系的生长，诱导了细胞凋亡[7]。
在体内，Vinorelbine ditartrate（30mg/kg）通过静脉注射治疗肺癌细胞系3LL细胞异种移植小鼠，几乎完全抑制了小鼠体内肿瘤生长和恶性胸腔积液（MPE）的产生，显著降低了肿瘤的新血管生成和血管内皮生长因子（VEGF）的表达[8]。
| Cell experiment [1]: | |
Cell lines | HOS and MG-63 osteosarcoma cell lines |
Preparation Method | Cells were treated with varying concentrations of Vinorelbine ditartrate for 8-72h. The drug concentration utilised ranged from 0.1 to 36nM. The effect of Vinorelbine ditartrate on the growth of HOS and MG-63 osteosarcoma cell lines was tested by SRB assay. |
Reaction Conditions | 0.1-36nM; 8-72h |
Applications | Vinorelbine ditartrate was found to inhibit the growth of each cell line in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | For intrapleural injection, C57BL/6 mice were anesthetized by intramuscular injection with 0.1mL of a mixture of ketamine and xylazine. The skin overlying the lateral chest wall was shaved and disinfected, and a 2 to 3mm-long transverse skin incision was made on the light infrascapular region. Ten thousand 3LL cells suspended in 100μL RPMI-1640 medium were injected into the pleural cavity through the intercostal space under direct observation. The mice were observed until complete recovery and this procedure was not associated with mortality or morbidity. Vinorelbine ditartrate (30mg/kg) or saline was administered once intravenously at day 8 after injection with 3LL cells. After day 13, mice were euthanized by diethylether. The abdominal wall was cut down, and the viscera were retracted to visualize the diaphragm. Pleural effusion (PE) was collected using a 1-mL syringe and the volume of PE was determined with the syringe. Thereafter, the chest wall was cut carefully with scissors and the intrapleural tumors were harvested. The tumors were washed with 0.9% saline and the weights of the tumors were determined with an automatic balance. |
Dosage form | 30mg/kg; i.v. |
Applications | Treatment with Vinorelbine ditartrate almost completely inhibited tumor growth and MPE production. In addition, immunohistochemical staining revealed that neovascularization and vascular endothelial growth factor (VEGF) expression were markedly decreased in Vinorelbine ditartrate-treated tumors compared with those of the control tumors. |
References: | |
| Cas No. | 125317-39-7 | SDF | |
| 别名 | 酒石酸长春瑞滨; KW-2307; Nor-5'-anhydrovinblastine ditartrate | ||
| 化学名 | Navelbine ditartrate;KW-2307;Nor-5'-anhydrovinblastine ditartrate | ||
| Canonical SMILES | CCC1=CC2CC(C3=C(CN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC.C(C(C(=O)O)O)(C(=O)O)O.C(C(C(=O)O)O)(C(=O)O)O | ||
| 分子式 | C53H66N4O20 | 分子量 | 1079.11 |
| 溶解度 | ≥ 33.7 mg/mL in DMSO, ≥ 41.9 mg/mL in EtOH with ultrasonic, ≥ 43 mg/mL in Water with ultrasonic | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 926.7 μL | 4.6334 mL | 9.2669 mL |
| 5 mM | 185.3 μL | 926.7 μL | 1.8534 mL |
| 10 mM | 92.7 μL | 463.3 μL | 926.7 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
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