| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Vinorelbine binds to tubulin, the protein subunit of microtubules, thereby inhibiting tubulin polymerization into microtubules. This disruption prevents the formation of the mitotic spindle during cell division, leading to metaphase arrest and ultimately apoptosis in rapidly dividing cancer cells. The mitotic blockage is concentration‑ and time‑dependent.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Vinorelbine inhibits the proliferation of HeLa cells in vitro with an IC50 of 1.25 nM. The deuterium‑labeled version is assumed to retain the same tubulin‑binding affinity and is used as a tracer in cellular uptake and efflux studies, as the deuterium substitution does not alter the parent molecule's primary chemical structure. |
| ln Vivo |
Vinorelbine exhibits dose‑dependent anti‑tumor activity in various xenograft models, including human lung cancer (A549) and breast cancer (MCF‑7) models. The compound reduces tumor growth by interfering with microtubule dynamics and inducing mitotic cell death. The deuterated version is not administered as a therapeutic itself but is used as an analytical tracer for pharmacokinetic studies in animals.
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| Enzyme Assay |
A competition binding assay using radiolabeled vinorelbine ([3H]‑vinorelbine) and purified tubulin or microtubule protein is performed. The test compound (vinorelbine‑d3) is incubated with tubulin (0.5 mg/mL) in PEM buffer (100 mM PIPES, 1 mM EGTA, 1 mM MgSO4, pH 6.9). After incubation at 37degC for 30 minutes, the reaction is filtered, and the bound radioactivity is counted. The IC50 is determined by non‑linear regression.
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| Cell Assay |
Human cancer cell lines (e.g., HeLa, A549, MCF‑7) are cultured in appropriate medium and treated with increasing concentrations of vinorelbine‑d3 (0.01‑100 nM) for 48‑72 hours. Cell viability is assessed by an MTT or CellTiter‑Glo assay. For cell cycle analysis, cells are fixed with ethanol, stained with propidium iodide, and analyzed by flow cytometry to quantify the accumulation of cells in the G2/M phase.
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| Animal Protocol |
Mice bearing subcutaneous tumor xenografts are treated intravenously or intraperitoneally with vinorelbine (2‑10 mg/kg) on a weekly schedule. Serial blood samples are collected, and plasma concentrations of vinorelbine and vinorelbine‑d3 (when used as an internal standard) are measured by LC‑MS/MS. Alternatively, tissue samples can be homogenized and analyzed to study drug distribution.
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| ADME/Pharmacokinetics |
Vinorelbine is moderately lipophilic and has a large volume of distribution (approximately 40 L/kg), indicating extensive tissue binding. It is highly (≈80‑90%) bound to plasma proteins, mainly to albumin and alpha1‑acid glycoprotein. The terminal elimination half‑life is relatively long (approximately 40 hours). The drug is primarily eliminated by CYP3A4‑mediated metabolism in the liver.
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| Toxicity/Toxicokinetics |
Vinorelbine clinically causes dose‑limiting neutropenia (low white blood cell counts) as its major adverse effect. Mild to moderate peripheral neuropathy, constipation, nausea, and alopecia can also occur. The deuterated version is not intended for human use and is used only in research settings at concentrations orders of magnitude below toxic levels.
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| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Ngan VK, et al. Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine. Mol Pharmacol. 2001 Jul;60(1):225-32. [3]. Liu XM, et al. Unique induction of p21(WAF1/CIP1)expression by vinorelbine in androgen-independent prostate cancer cells. Br J Cancer. 2003 Oct 20;89(8):1566-73. [4]. Poirier VJ, et al. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9. [5]. Pierro JA, et al. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8. |
| Additional Infomation |
Vinorelbine (Navelbine) received FDA approval in 1994 for non‑small cell lung cancer and later for breast cancer. It is administered intravenously, often in combination with other chemotherapeutic agents (e.g., cisplatin). Vinorelbine‑d3 ditartrate serves as a stable isotope internal standard for the quantification of vinorelbine in biological matrices, enabling high‑throughput bioanalytical assays for therapeutic drug monitoring and pharmacokinetic studies.
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| Molecular Formula |
C53H63D3N4O20
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|---|---|
| Related CAS # |
Vinorelbine ditartrate;125317-39-7
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~92.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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