Vinorelbine Tartrate

Catalog No.S4269

Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin.

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Vinorelbine Tartrate Chemical Structure

Vinorelbine Tartrate Chemical Structure
Molecular Weight: 1079.11

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Product Information

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Product Description

Biological Activity

Description Vinorelbine Tartrate is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin.
Targets Tubulin [1]
(Cell-free assay)
In vitro Vinorelbine inhibits microtubule assembly by inducing tubulin aggregation into spirals and paracrystals. [1] Vinorelbine shows potent antiproliferative activity against a series of tumor cells, including human melanoma, non-small-cell lung cancer, breast cancer, etc. [2][3][4]
In vivo In vivo, Vinorelbine also shows antitumour activity against a series of subcutaneously-implanted human tumour xenografts. [5]
Features A semi-synthetic vinca alkaloid as an anti-mitotic chemotherapy drug.

Protocol(Only for Reference)

Animal Study: [5]

Animal Models Bladder (BXF1299), pancreas (PAXF546), kidney (RXF944LX), colon (DLD-1, HT-29, TC37), central nervous system (SF-295), small cell lung (NCI-H69) and prostate (PC-3) xenografts.
Formulation Sterile 0.9% sodium chloride solution
Dosages ~10 mg/kg
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Fellous A, et al. Semin Oncol. 1989, 16(2 Suppl 4), 9-14.

[2] Photiou A, et al. J Cancer Res Clin Oncol. 1992, 118(4), 249-254.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02574455 Not yet recruiting Breast Cancer Immunomedics, Inc. July 2016 Phase 3
NCT02733380 Recruiting Diffuse Large B-cell Lymphoma Henan Cancer Hospital May 2016 Phase 2
NCT02658084 Not yet recruiting Breast Cancer|Metastatic Breast Cancer University of Miami|Genentech, Inc. March 2016 Phase 1|Phase 2
NCT02709720 Not yet recruiting Lung Cancer Spanish Lung Cancer Group March 2016 Phase 2
NCT02619929 Recruiting Non-Small-Cell Lung Cancer|Breast Cancer Pierre Fabre Pharma GmbH|Winicker Norimed GmbH February 2016 --

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Chemical Information

Download Vinorelbine Tartrate SDF
Molecular Weight (MW) 1079.11
Formula

C45H54N4O8.2C4H6O6

CAS No. 125317-39-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (92.66 mM)
Water 100 mg/mL warmed (92.66 mM)
Ethanol 100 mg/mL warmed (92.66 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 3',4'-Didehydro-4'-deoxy-C'-norvincaleukoblastine ditartrate

Customer Product Validation (1)


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Rating
Source Cynthia Bernia from McGill University. Vinorelbine Tartrate purchased from Selleck
Method Cells viability assay
Cell Lines NCl-H23/NCl-H460/HCC44 cell lines
Concentrations 0-10000 nM
Incubation Time
Results It examined responsiveness to vinorelbine, which can inhibit mitosis through interaction with tubulin. The results suggsted that vinorebine inhibited NSCLC cells in different concentration, that demonstrated sensitivity to vinorelbine at clinically useful concentrations (EC50 from 8.092 nM to 1.363 nM) in the majority of cell lines tested.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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