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Vinorelbine ditartrate (KW-2307)

Alias:
Cat No.:V1615 Purity: ≥98%
Vinorelbine ditartrate (KW-2307; KW2307;Navelbine, Biovelbin, Eunades; Nor-5-anhydrovinblastine), the ditartrate salt of vinorelbine which is an antimitotic agent, is a tubulin inhibitor and microtubule stablizer approved for cancer treatment.
Vinorelbine ditartrate (KW-2307)
Vinorelbine ditartrate (KW-2307) Chemical Structure CAS No.: 125317-39-7
Product category: Microtubule Associated
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Vinorelbine ditartrate (KW-2307; KW2307; Navelbine, Biovelbin, Eunades; Nor-5'-anhydrovinblastine), the ditartrate salt of vinorelbine which is an antimitotic agent, is a tubulin inhibitor and microtubule stablizer approved for cancer treatment. It is a semisynthetic vinca alkaloid derived from the leaves of the periwinkle plant (Vinca rosea) and has been used extensively for the treatment for various cancers such as breast cancer and non-small cell lung cancer.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Cell proliferation is 50% (IC50) inhibited by vinorelbine (0.5–5 nM) ditartrate at 1.25 nM. No cells are in anaphase at a concentration of 8 nM [1]. In both androgen-dependent (AD) and androgen-independent (AI) prostate cancer cell lines, vinorelbine ditartrate time-dependently induces the expression of p53 and p21WAFI/CIP1. Reporter gene stimulation by vinorelbine ditartrate is concentration-dependent [2].
ln Vivo
In vivo, Vinorelbine also shows antitumour activity against a series of subcutaneously-implanted human tumour xenografts.
Animal Protocol
Dissolved in Sterile 0.9% sodium chloride solution; 10 mg/kg; i.p. injection
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.
References

[1]. 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]. 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]. Toxicity, dosage, and efficacy of vinorelbine (Navelbine) in dogs with spontaneous neoplasia. J Vet Intern Med. 2004 Jul-Aug;18(4):536-9.

[4]. Phase I clinical trial of vinorelbine in tumor-bearing cats. J Vet Intern Med. 2013 Jul-Aug;27(4):943-8.

Additional Infomation
Vinorelbine Tartrate is the ditartrate salt of a semisynthetic vinca alkaloid derived from the leaves of the periwinkle plant (Vinca rosea) with antineoplastic properties. Vinorelbine binds to tubulin, thereby inhibiting tubulin polymerization into microtubules and spindle formation and resulting in apoptosis of susceptible cancer cells. Inhibition of mitotic microtubules correlates with antitumor activity, whereas inhibition of axonal microtubules seems to correlate with vinorelbine's neurotoxicity. Compared to related vinca alkaloids, vinorelbine is more selective against mitotic than axonal microtubules in vitro, which may account for its decreased neurotoxicity. This agent is also a radiation-sensitizing agent. (NCI04)
Liposomal Vinorelbine Tartrate is a formulation of the tartrate salt form of vinorelbine, a semisynthetic vinca alkaloid, encapsulated within liposomes, with potential antineoplastic activity. Upon intravenous administration, vinorelbine binds to tubulin within tumor cells and prevents the formation of the mitotic spindle, resulting in cell cycle arrest, induction of apoptosis and an inhibition of tumor cell growth. Compared to the administration of vinorelbine alone, the liposomal formulation improves drug penetration into tumors and decreases drug clearance, thereby increasing vinorelbine's efficacy while lowering the toxicity profile.
A vinca alkaloid related to VINBLASTINE that is used as a first-line treatment for NON-SMALL CELL LUNG CANCER, or for advanced or metastatic BREAST CANCER refractory to treatment with ANTHRACYCLINES.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C45H54N4O8.2C4H6O6
Molecular Weight
1079.11
Exact Mass
1078.427
CAS #
125317-39-7
Related CAS #
Vinorelbine-d3 ditartrate
PubChem CID
16051941
Appearance
White to off-white solid powder
Density
1.36g/cm3
Melting Point
181-183°C
Index of Refraction
1.675
LogP
0.449
Hydrogen Bond Donor Count
10
Hydrogen Bond Acceptor Count
23
Rotatable Bond Count
16
Heavy Atom Count
77
Complexity
1820
Defined Atom Stereocenter Count
8
SMILES
CCC1=C[C@H]2C[C@@](C3=C(CN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)[C@]78CCN9[C@H]7[C@@](C=CC9)([C@H]([C@@]([C@@H]8N6C)(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
InChi Key
CILBMBUYJCWATM-PYGJLNRPSA-N
InChi Code
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
Chemical Name
methyl (3aR,3a1R,4R,5S,5aR,10bR)-4-acetoxy-3a-ethyl-9-((6R,8S)-4-ethyl-8-(methoxycarbonyl)-1,3,6,7,8,9-hexahydro-2,6-methanoazecino[4,3-b]indol-8-yl)-5-hydroxy-8-methoxy-6-methyl-3a,3a1,4,5,5a,6,11,12-octahydro-1H-indolizino[8,1-cd]carbazole-5-carboxylate bis((2R,3R)-2,3-dihydroxysuccinate)
Synonyms

KW2307, Nor-5''-anhydrovinblastine ditartrate, vinorelbine tartrate, KW-2307, KW 2307,Navelbine, Biovelbin, Eunades

HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:100 mg/mL (92.7 mM)
Water:100 mg/mL (92.7 mM)
Ethanol:100 mg/mL (92.7 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.08 mg/mL (1.93 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: 2.08 mg/mL (1.93 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 50 mg/mL (46.33 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

Solubility in Formulation 5: 20 mg/mL (18.53 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.9267 mL 4.6334 mL 9.2669 mL
5 mM 0.1853 mL 0.9267 mL 1.8534 mL
10 mM 0.0927 mL 0.4633 mL 0.9267 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03443128 RECRUITING Drug: Vinorelbine Vinorelbine
Anaplastic Large Cell Lymphoma
Children's Cancer
Group, China
2016-11 Phase 2
NCT02544243 UNKNOWN STATUS Drug: Vinorelbine
Drug: Gemcitabine
Drug: Cisplatin
Metastatic Breast Cancer Shandong Cancer
Hospital and Institute
2015-09 Phase 2
NCT05296577 RECRUITING Drug:anlotinib and vinorelbine
Drug:Vinorelbine injection
Breast Cancer Henan Cancer Hospital 2022-03-22 Phase 2
Biological Data
  • Time-dependent induction of p53 and p21WAFI/CIP1 expression in androgen-dependent (AD) and- independent (AI) prostate cancer cell lines by vinorelbine. Androgen-independent and AI cells grown exponentially were exposed to 0.1 μm of vinorelbine for indicated periods of time. The cells were harvested, washed, and total proteins extracted. Proteins (50 μg) were subjected to 4/10% stacking SDS–PAGE, electrotransferred to nitrocellulose membrane, and immunoblotted with p21WAFI/CIP1 and p53 monoclonal antibodies, respectively. The same membrane was stripped, and reprobed with antibody against β-actin for equal loading control. Br J Cancer . 2003 Oct 20;89(8):1566-73.
  • Effects of paclitaxel (left panel) and vinorelbine (middle and right panel) on the expression of p53 and p21WAFI/CIPI in androgen-dependent (AD, left and middle panel) and-independent (AI, right panel) prostate cancer cell lines. AD and AI cells grown exponentially were exposed for 24 h to different concentrations of paclitaxel (left panel) or vinorelbine (middle and right). The cells were harvested, washed, and total proteins extracted. Fifty μg of proteins were subjected to 4%/10% stacking SDS-PAGE, electrotransferred to nitrocellulose membrane, and immunoblotted with p21WAFI/CIPI and p53 monoclonal antibodies, respectively. The same membrane was stripped and reprobed using antibody against β-actin for equal loading control. Br J Cancer . 2003 Oct 20;89(8):1566-73.
  • Synergistic effects of sequential combination of paclitaxel and vinorelbine in AD and AI cells. Androgen-dependent and AI cells at exponential growth phase in 96-well dishes were exposed to a series dilution of either paclitaxel (TAX) or vinorelbine (NBV) alone for 7 days or paclitaxel for 3 days followed by paclitaxel plus vinorelbine for additional 4 days. Cell growth was determined by MTT, and the combination indexes (CI) were calculated by a PC program CalcuSyn as described in the Materials and Methods. Panels A and B, the effect–concentration plots in AD (A) and AI (B); Panels C and D, the effect –combination index plots in AD (C) and AI (D). Panel E: the expression of p53 and p21 in AD and AI cells after exposure for 24 h to NVB or TAX alone or NVB plus TAX. Br J Cancer . 2003 Oct 20;89(8):1566-73.
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