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Vinorelbine Tartrate

Anti-mitotic chemotherapy drug CAS# 125317-39-7

Vinorelbine Tartrate

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Vinorelbine Tartrate:5mg $55.00 In Stock
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Quality Control of Vinorelbine Tartrate

Number of papers citing our products

Chemical structure

Vinorelbine Tartrate

3D structure

Chemical Properties of Vinorelbine Tartrate

Cas No. 125317-39-7 SDF Download SDF
PubChem ID 60779 Appearance Powder
Formula C53H66N4O20 M.Wt 1079.11
Type of Compound Alkaloids Storage Desiccate at -20°C
Synonyms Navelbine
Solubility DMSO : ≥ 46 mg/mL (42.63 mM)
*"≥" means soluble, but saturation unknown.
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
Standard InChIKey CILBMBUYJCWATM-NPJYPKOYSA-N
Standard InChI InChI=1S/C45H54N4O8.2C4H6O6/c1-8-27-19-28-22-44(40(51)55-6,36-30(25-48(23-27)24-28)29-13-10-11-14-33(29)46-36)32-20-31-34(21-35(32)54-5)47(4)38-43(31)16-18-49-17-12-15-42(9-2,37(43)49)39(57-26(3)50)45(38,53)41(52)56-7;2*5-1(3(7)8)2(6)4(9)10/h10-15,19-21,28,37-39,46,53H,8-9,16-18,22-25H2,1-7H3;2*1-2,5-6H,(H,7,8)(H,9,10)/t28?,37-,38+,39+,42+,43+,44-,45-;2*1-,2-/m011/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Source of Vinorelbine Tartrate

The herbs of Catharanthus roseus

Biological Activity of Vinorelbine Tartrate

DescriptionVinorelbine Tartrate is an antitumor drug.
TargetsImmunology & Inflammation related
In vitro

Visual, turbidimetric, and particle-content assessment of compatibility of vinorelbine tartrate with selected drugs during simulated Y-site injection.[Pubmed: 8017415]

Am J Hosp Pharm. 1994 Feb 15;51(4):495-9.

The compatibility of Vinorelbine Tartrate with selected drugs during simulated Y-site administration was studied.
METHODS AND RESULTS:
A 5-mL sample of Vinorelbine Tartrate 1 mg/mL in 0.9% sodium chloride injection was combined with a 5-mL sample of each of 91 other drugs at concentrations used clinically. Each combination was prepared in duplicate, with the order of mixing being reversed between the two; storage was in constant fluorescent light at 22 degrees C. The admixtures were examined visually in normal fluorescent light and with a Tyndall beam at zero, one, and four hours after preparation. A turbidimeter was used to measure the turbidity of each drug combination at the same intervals. Samples showing visual or turbidimetric evidence of incompatibility were subjected to particle counting and sizing. The majority of the drugs tested were compatible with Vinorelbine Tartrate; most combinations had a turbidity of less than 0.1 nephelometric turbidity unit. Turbidity measurements showed that cefazolin sodium, ceforanide, and cefuroxime sodium were incompatible with Vinorelbine Tartrate. Visual observation showed incompatibility of Vinorelbine Tartrate with acyclovir sodium, aminophylline, amphotericin B, ampicillin sodium, cefoperazone sodium, ceforanide, cefotetan sodium, ceftriaxone sodium, fluorouracil, furosemide, ganciclovir sodium, methylprednisolone sodium succinate, mitomycin, piperacillin sodium, sodium bicarbonate, thiotepa, and trimethoprimsulfamethoxazole.
CONCLUSIONS:
Vinorelbine Tartrate 1 mg/mL in 0.9% sodium chloride injection was compatible with the majority of the drugs tested for up to four hours at 22 degrees C but was incompatible with 19 drugs.

In vivo

Vinorelbine Tartrate-Induced Pulmonary Edema Confirmed on Rechallenge[Reference: WebLink]

Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy Volume 19, Issue 8, pages 992–994, August 1999

A 67-year-old woman with metastatic breast cancer experienced sudden and profound pulmonary edema within 45 minutes after completion of intravenous administration of Vinorelbine Tartrate on two occasions. Both times the drug was discontinued and the patient was treated aggressively with oxygen, intravenous furosemide, and a vasodilator. The patient suffered no lasting medical complications due to the reaction. Until clear documentation and the mechanism for occurrence of this reaction are known, patients receiving vinorelbine should be monitored closely, particularly in the first few hours after intravenous administration.

The Protection Effects of Matrine on Vinorelbine Tartrate Induced Venous Injury[Reference: WebLink]

《Journal of Ningxia Medical University》 2010-07

To explore the protection effect of the Matrine on antitumor drug-Vinorelbine Tartrate Injection induced venous injury.
METHODS AND RESULTS:
The auricular venous injury model of rabbits was established by intravenous infusion of VTI.Different methods were selected to treat the injury: applying Matrine and applying MgSO4.The injury status of the veins and peripheral tissues were observed and HE stain were performed after 48 hours and 7 days treatment,respectively.the histopathological features of the veins and peripheral tissues were analyzed. After comparing the histopathological results of the samples among the 3 groups,the venous injury of the Matraine group was the least severe one in aspect of Lumen hyperemia,inflammatory cell infiltration,bleeding of the perivascular for past 48 hours treatment(P0.05);for post 7days treatment,the venous injury of the Matraine group was the least severe one in aspect of inflammatory cell infiltration,bleedingof the perivascular(P0.05);the subsidence of the venous injury of the Matraine group was the earliest one(P=0.000).
CONCLUSIONS:
Matrine is an effective method on prevention of the antitumor drug Vinorelbine Tartrate induced venous injury.

Protocol

Animal Administration [4]
As defined by the study, VRL1 is diluted in 0.9% NaCl to a concentration of 1.5 mg/mL, and given IV over 5 minutes. The intended treatment interval is 7 days for up to 4 treatments. After receiving 4 weekly doses, cats are eligible to continue VRL treatment every 2 weeks.

References:
[1]. 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. [2]. 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. [3]. 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. [4]. 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.

Vinorelbine Tartrate Dilution Calculator

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Vinorelbine Tartrate Molarity Calculator

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Preparing Stock Solutions of Vinorelbine Tartrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 0.9267 mL 4.6334 mL 9.2669 mL 18.5338 mL 23.1672 mL
5 mM 0.1853 mL 0.9267 mL 1.8534 mL 3.7068 mL 4.6334 mL
10 mM 0.0927 mL 0.4633 mL 0.9267 mL 1.8534 mL 2.3167 mL
50 mM 0.0185 mL 0.0927 mL 0.1853 mL 0.3707 mL 0.4633 mL
100 mM 0.0093 mL 0.0463 mL 0.0927 mL 0.1853 mL 0.2317 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Vinorelbine Tartrate

Description: IC50 Value: 1.25 nM (Hela cell) [1] Vinorelbine is an anti-mitotic chemotherapy drug that is given as a treatment for some types of cancer, including breast cancer and non-small cell lung cancer. in vitro: 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: Nineteen dogs were treated with vinorelbine as a 5-minute IV infusion every 7 days at starting dosages ranging from 10 to 20 mg/m2. The median number of treatments per dog was 7 (range, 1-11). The maximum tolerated dosage varied between 15 and 18 mg/m2, and a starting dosage of 15 mg/m2 is recommended [3]. Sixty-one VRL treatments were administered. Median number of treatments was 2 (range, 1-9). Starting dosages were 9-12 mg/m(2) . Maximal dosage administered was 15.5 mg/m(2) . The MTD was 11.5 mg/m(2) . Acute DLTs were neutropenia, vomiting, and nephrotoxicity. Other notable toxicities were weight loss and anemia [4]. Toxicity: Acute DLTs were neutropenia, vomiting, and nephrotoxicity. Other notable toxicities were weight loss and anemia [4]. Clinical trial: XeNa: Phase II Trial With Metronomic, Capecitabine Plus Oral Vinorelbine for Metastatic Breast Cancer. Phase 2

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References on Vinorelbine Tartrate

Visual, turbidimetric, and particle-content assessment of compatibility of vinorelbine tartrate with selected drugs during simulated Y-site injection.[Pubmed:8017415]

Am J Hosp Pharm. 1994 Feb 15;51(4):495-9.

The compatibility of Vinorelbine Tartrate with selected drugs during simulated Y-site administration was studied. A 5-mL sample of Vinorelbine Tartrate 1 mg/mL in 0.9% sodium chloride injection was combined with a 5-mL sample of each of 91 other drugs at concentrations used clinically. Each combination was prepared in duplicate, with the order of mixing being reversed between the two; storage was in constant fluorescent light at 22 degrees C. The admixtures were examined visually in normal fluorescent light and with a Tyndall beam at zero, one, and four hours after preparation. A turbidimeter was used to measure the turbidity of each drug combination at the same intervals. Samples showing visual or turbidimetric evidence of incompatibility were subjected to particle counting and sizing. The majority of the drugs tested were compatible with Vinorelbine Tartrate; most combinations had a turbidity of less than 0.1 nephelometric turbidity unit. Turbidity measurements showed that cefazolin sodium, ceforanide, and cefuroxime sodium were incompatible with Vinorelbine Tartrate. Visual observation showed incompatibility of Vinorelbine Tartrate with acyclovir sodium, aminophylline, amphotericin B, ampicillin sodium, cefoperazone sodium, ceforanide, cefotetan sodium, ceftriaxone sodium, fluorouracil, furosemide, ganciclovir sodium, methylprednisolone sodium succinate, mitomycin, piperacillin sodium, sodium bicarbonate, thiotepa, and trimethoprimsulfamethoxazole. Vinorelbine Tartrate 1 mg/mL in 0.9% sodium chloride injection was compatible with the majority of the drugs tested for up to four hours at 22 degrees C but was incompatible with 19 drugs.

The effects of vinflunine, vinorelbine, and vinblastine on centromere dynamics.[Pubmed:12748304]

Mol Cancer Ther. 2003 May;2(5):427-36.

Vinflunine is a novel fluorinated Vinca alkaloid currently in Phase II clinical trials, which in preclinical studies exhibited superior antitumor activity to that of two clinically useful Vinca alkaloids, vinorelbine and vinblastine. All three of the drugs block mitosis at the metaphase/anaphase transition, leading to apoptosis. The mechanism of the mitotic block is not known. On the basis of results with purified microtubules and in living interphase cells, we hypothesized that it involves suppression of spindle microtubule dynamics. Here we measured the effects of the three Vinca alkaloids on dynamics of centromeres and spindle kinetochore-microtubules by a novel approach involving quantitative time-lapse confocal microscopy in living mitotic human U2OS cells. Green fluorescent protein-labeled centromere-binding protein B was used to mark centromeres and kinetochore-microtubule plus ends. In controls, pairs of centromeres on sister chromatids alternated under tension between increasing and decreasing separation (stretching and relaxing). All three of the Vinca alkaloids suppressed centromere dynamics similarly at concentrations that block mitosis. At concentrations approximating the IC(50)s for mitotic accumulation (18.8 nM vinflunine, 7.3 nM vinorelbine, and 6.1 nM vinblastine), centromere dynamicity decreased by 44%, 25%, and 26%, respectively, and the time centromeres spent in a paused state increased by 63%, 52%, and 36%, respectively. Centromere relaxation rates, stretching durations, and transition frequencies all decreased. Thus all three of the drugs decreased the normal microtubule-dependent spindle tension at the centromeres/kinetochores, thereby preventing the signal for mitotic checkpoint passage. The strong correlation between suppression of kinetochore-microtubule dynamics and mitotic block indicates that the primary mechanism by which the Vinca alkaloids block mitosis is suppression of spindle microtubule dynamics.

Mechanism of mitotic block and inhibition of cell proliferation by the semisynthetic Vinca alkaloids vinorelbine and its newer derivative vinflunine.[Pubmed:11408618]

Mol Pharmacol. 2001 Jul;60(1):225-32.

The two second-generation Vinca alkaloids, vinorelbine and vinflunine, affect microtubule dynamics very differently from vinblastine, a first generation Vinca alkaloid. For example, vinblastine strongly suppresses the rate and extent of microtubule shortening in vitro, whereas vinorelbine and vinflunine suppress the rate and extent of microtubule growing events. We asked whether these differences result in differences in mitotic spindle organization that might be responsible for the superior antitumor activities of the two second-generation Vinca alkaloids. IC(50) values for inhibition of HeLa cell proliferation for vinflunine, vinorelbine, and vinblastine were 18, 1.25, and 0.45 nM, respectively, similar to the concentrations that induced mitotic block at the metaphase/anaphase transition (38, 3.8, and 1.1 nM, respectively), indicating that mitotic block is a major contributor to antiproliferative action for all three drugs. Mitotically blocked cells exhibited aberrant spindles, consistent with induction of block by suppression of microtubule dynamics. Despite differences in their actions on individual dynamic instability parameters, morphologically detectable differences in spindle effects among the three drugs were minimal, indicating that overall suppression of dynamics may be more important in blocking mitosis than specific effects on growth or shortening. We also found that the peak intracellular drug concentration at the mitotic IC(50) value was highest for vinflunine (4.2 +/- 0.2 microM), intermediate for vinorelbine (1.3 +/- 0.1 microM), and more than 10-fold lower for vinblastine (130 +/- 7 nM), suggesting that intracellular binding reservoir(s) may be partially responsible for vinflunine's high efficacy and minimal side effects.

Vinorelbine (Navelbine): a third-generation vinca alkaloid.[Pubmed:9316630]

Cancer Invest. 1997;15(5):475-90.

The vinca alkaloids represent one of the oldest classes of antineoplastic agents used in humans with a wide spectrum of activity against both animal and human tumors. These agents are known to inhibit microtubule polymerization. Vinorelbine is a semisynthetic analog that reached clinical trial on the basis of less preclinical evidence of toxicity to neuronal tissue and greater cytotoxic activity in preclinical models than the older compounds of this class. In humans, the clearance of this agent shows a wide variation among subjects with the predominant toxicity being hematological. Significant antitumor activity has been observed in diseases that previously have been shown to respond to vinca alkaloids.

Description

Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.

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