Antibodies
Vinorelbine
- 貨號 Cat. No.
- S1527
- 規格 Size
- 10mgã€50mg
- 品牌 Brand
- Selleckchem
Description
Vinorelbine
Catalog No.S1527
Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Vinorelbine is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM. | |||||
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| Targets | Anti-mitotic (Hela cells) | |||||
| IC50 | 1.25 nM [1] | |||||
| In vitro | Vinorelbine, a semisynthetic derivative of vinca alkaloid, is effective in non–small-cell lung cancer, metastatic breast cancer, and ovarian cancer and shows promise in lymphoma, esophageal cancer, and prostatic carcinoma. Vinorelbine, more significantly, inhibits the proliferation of HeLa cells with IC50 of 1.25 nM, compared to vinflunine with IC50 of 18 nM. Vinorelbine blocks cell cycle progression in mitosis with IC50 of 3.8 nM, which is only slightly higher than the IC50 value for inhibition of proliferation, indicating that mitotic block is a major contributor to antiproliferative action. Vinorelbine has the greatest effect, 29%, on reduction of the spindle length compared to 20% by vinflunine and 22% by vinblastine at the IC50 concentrations of the three drugs. [1]Vinorelbine induces concentration- and time-dependent increases in the protein levels of both p53 and p21 in hormone-dependent (AD) LNCaP cells, and can restore p21 expression in androgen-independent (AI) prostate cancer cells through both p53-dependent and-independent pathways. [2] | |||||
| In vivo | Vinorelbine treatment at 2.5 and 5 mg/kg significantly increases the median survival time (MST) of NCI-H460 tumor bearing mice from 21 days to 24 and 35 days, respectively. Vinorelbine in combination with the Bcl-2 antisense oligonucleotide oblimersen induces highly significant tumor growth suppression in a dose-dependent manner than either drug used alone and without showing significant signs of undesirable toxicity. [3]Administration of Vinorelbine at a dose of 3 mg/kg once weekly for 6 weeks produces 22% reduction in the tumor volume of human breast cancer xenografts in athymic mice. The anticancer activity can be significantly enhanced in combination with 2-MeO-E2 (30 mg/kg) with tumor growth almost completely inhibited during the first 2 weeks. [4] | |||||
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Protocol(Only for Reference)
Cell Assay: [1]
| Cell lines | HeLa cells |
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| Concentrations | 0.5-5 nM |
| Incubation Time | 20 hours |
| Method | Hela cells are exposed to Vinorelbine (0.5-5 nM) for 20 hours. Live cells are counted using a hemocytometer, with trypan blue dye beimg used to distinguish living from dead cells. Cell proliferation is calculated from the difference in cell number at the beginning and at the end of the Vinorelbine incubation, relative to the increase in cell number for control cultures during the same period. For the determination of mitotic index, both detached and attached cells are collected, fixed, and their microtubules and chromosomes stained. The numbers of cells in mitosis and in interphase are then determined by microscopy. |
Animal Study: [3]
| Animal Models | Male severe combined immunodeficient (SCID)-RAG2 mice implanted with NCI-H460 cells subcutaneously or through the chest wall into the left pleural space |
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| Dosages | 5 or 10 mg/kg |
| Administration | Intravenously every 4th day |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01635465 | Not yet recruiting | Anthracycline-pretreated Metastatic Breast Cancer | Tianjin Medical University Cancer Institute and Hospital | 2013-08 | |
| NCT01950182 | Recruiting | Breast Cancer | Sun Yat-sen University | 2013-09 | Phase 3 |
| NCT01945775 | Recruiting | Breast Neoplasms|BRCA 1 Gene Mutation|BRCA 2 Gene Mutation | BioMarin Pharmaceutical|National Breast Cancer Coalition (NBCC)|Translational Research In Oncology (TRIO)|US Oncology Research | 2013-10 | Phase 3 |
| NCT02004184 | Not yet recruiting | Carcinoma, Non-small-cell Lung | Norwegian University of Science and Technology|St. Olavs Hospital | 2013-12 | Phase 3 |
| NCT02000622 | Not yet recruiting | Breast Cancer Metastatic | AstraZeneca | 2014-03 | Phase 3 |
Chemical Information
| Molecular Weight (MW) | 778.93 |
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| Formula | C45H54N4O8 |
| CAS No. | 71486-22-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (128 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 13 mg/mL (16 mM) | ||
| * <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 | Aspidospermidine-3-carboxylic acid, 4-(acetyloxy)-6,7-didehydro-15-[(2R,6R,8S)-4-ethyl-1,3,6,7,8,9-hexahydro-8-(methoxycarbonyl)-2,6-methano-2H-azecino[4,3-b]indol-8-yl]-3-hydroxy-16-methoxy-1-methyl-, methyl ester, (2β,3β,4β,5α,12R,19α)- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.77893 | 7.7893 | 15.5786 | 23.3679 |
