| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
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Purity: ≥98%
Vinblastine sulfate (also known as NSC49842; Vincaleukoblastine), a natural alkaloid extracted from the plant Vinca rosea Linn, is an approved anticancer drug and a potent mitotic inhibitor that inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, it is used to treat certain kinds of cancer. Vinblastine binds to tubulin and prevents the formation of microtubules, which disrupts the assembly of mitotic spindles and stops tumor cells in the M phase of the cell cycle.
| Targets |
nAChR (IC50 = 8.9 μM)
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| ln Vitro |
Vinblastine is a potent mitotic inhibitor (IC50 0.8 nM in HeLa cells), preventing cell death through apoptosis while not depolymerizing spindle microtubules[2]. Vinblastine causes p53 alteration and DNA fragmentation in NB4 cells. By inducing apoptosis and causing a Bax/Bcl-2 imbalance, vinblastine treatment has an antiproliferative effect. Treatment with vinblastine inhibits NFκB expression and decreases NFκB-DNA binding activity, all the while preserving JNK activation, which in turn triggers an apoptotic response via a caspase-dependent pathway[3]. Apoptosis inducing factor and cytochrome c release, cleavage of poly (ADP-ribose)-Polymerase, activation of caspase-9 and 3, and loss of mitochondrial membrane potential are all signs that vinblastine induces apoptosis[4].
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| ln Vivo |
Vinblastine is a popular anticancer medication that has unfavorable side effects. One effective way to lessen these side effects might be to conjugate it with carrier molecules[5].
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| Cell Assay |
Six-well treatment plates are prepared with 5 × 104 cells/mL in each well, suspended in 3 mL culture medium, and treated with vinblastine for three hours, followed by a growth period of twenty-one hours.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C46H60N4O13S
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|---|---|
| Molecular Weight |
909.05
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| Exact Mass |
908.38776
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| Elemental Analysis |
C, 60.78; H, 6.65; N, 6.16; O, 22.88; S, 3.53
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| CAS # |
143-67-9
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| Related CAS # |
143-67-9 (sulfate);865-21-4 (free);
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| Appearance |
White to slight yellow solid powder
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| SMILES |
CC[C@@]1(C[C@@H]2C[C@@](C3=C(CCN(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)O.OS(=O)(=O)O
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| InChi Key |
KDQAABAKXDWYSZ-JKDPCDLQSA-N
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| InChi Code |
InChI=1S/C46H58N4O9.H2O4S/c1-8-42(54)23-28-24-45(40(52)57-6,36-30(15-19-49(25-28)26-42)29-13-10-11-14-33(29)47-36)32-21-31-34(22-35(32)56-5)48(4)38-44(31)17-20-50-18-12-16-43(9-2,37(44)50)39(59-27(3)51)46(38,55)41(53)58-7;1-5(2,3)4/h10-14,16,21-22,28,37-39,47,54-55H,8-9,15,17-20,23-26H2,1-7H3;(H2,1,2,3,4)/t28-,37+,38-,39-,42+,43-,44-,45+,46+;/m1./s1
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| Chemical Name |
methyl (1R,9R,10S,11R,12R,19R)-11-acetyloxy-12-ethyl-4-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-methoxycarbonyl-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraen-13-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carboxylate;sulfuric acid
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| Synonyms |
Vincaleucoblastine; VLB; Velsar; Velban
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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 |
| 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 (~110 mM)
Water: ~50 mg/mL (~55 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.75 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 (2.75 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 (2.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (55.00 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1000 mL | 5.5002 mL | 11.0005 mL | |
| 5 mM | 0.2200 mL | 1.1000 mL | 2.2001 mL | |
| 10 mM | 0.1100 mL | 0.5500 mL | 1.1000 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.
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03331341 | Active Recruiting |
Drug: Dacarbazine Drug: Vinblastine |
Classical Hodgkin Lymphoma | University of Washington | January 9, 2019 | Phase 2 |
| NCT03233347 | Active Recruiting |
Drug: Vinblastine Biological: Nivolumab |
Classic Hodgkin Lymphoma Ann Arbor Stage IIB Hodgkin Lymphoma |
Academic and Community| October 13, 2017 |
Phase 2 |
|
| NCT02670707 | Recruiting | Drug: Cytarabine Drug: Vinblastine/prednisone |
Langerhans Cell Histiocytosis | Baylor College of Medicine | March 7, 2016 | Phase 3 |
| NCT05062278 | Recruiting | Drug: Hydroxyurea capsules Drug: Vinblastine |
AML Hyperleukocytosis |
Hospital Universitario Dr. Jose E. Gonzalez |
July 26, 2021 | Phase 2 |
| NCT02840409 | Recruiting | Drug: Vinblastine Drug: Bevacizumab |
Low Grade Glioma | The Hospital for Sick Children | August 2016 | Phase 2 |
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