| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Vinflunine ditartrate (F 12158, BMS 710485) is a new analog of the vinca alkaloid vinorelbine that is bi-fluorinated strucuturally. It has anticancer, anti-angiogenic, vascular-disrupting, and anti-metastatic qualities as a mitotic or tubulin inhibitor. Vinflunine primarily slows down the rate of microtubule growth, lengthens the duration of growth, and shortens the duration of shortening in relation to dynamic instability. Vinflunine's effects on the readmilling rate are investigated by inserting [3H]GTP into MAP-rich microtubules; the IC50 is 0.42 μM.
| Targets |
Tubulin
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|---|---|---|---|
| ln Vitro |
Vinorelbine causes tubulin to aggregate into spirals and paracrystals, which prevents the formation of microtubules.[1]
Vinorelbine shows potent antiproliferative properties against various tumor cells, such as human melanoma, breast cancer, non-small-cell lung cancer, etc. [2][3][4] |
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| ln Vivo |
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| Enzyme Assay |
Purified tubulin (17 μM) is polymerized into microtubules using sea urchin (Strongylocentrotus purpuratus) axonemes as seeds for assembly initiation in 75 mM PIPES, 1.8 mM MgCl2, 1.0 mM EGTA, and 1.5 mM GTP, either in the absence or presence of a range of flunine concentrations (35 minutes; 37 °C). Centrifugation (150,000 × g; 1 hour; 35 °C) is used to separate polymerized microtubules from unpolymerized tubulin after incubation. After aspirating the supernatant and putting the sedimented microtubules in assembly buffer for two hours on ice to depolymerize them, the protein content is calculated.
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| Cell Assay |
Vinflunine's effects on the proliferation of L1210 cells are assessed using a common growth inhibition test. After being exposed to various concentrations of test compounds for 48 hours, exponentially growing L1210 cells (1.5 × 105 cells/well) in a 24-well plate are counted using an electronic particle counter that uses linear interpolation between data points to determine the number of cells.
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| Animal Protocol |
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| References |
| Molecular Formula |
C53H66F2N4O20
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|---|---|---|
| Molecular Weight |
1079.11
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| Exact Mass |
1078.43
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| Elemental Analysis |
C, 66.16; H, 6.66; F, 4.65; N, 6.86; O, 15.67
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| CAS # |
194468-36-5
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| Related CAS # |
194468-36-5 (ditartrate);162652-95-1;
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| Appearance |
White to off-white solid powder
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| SMILES |
CC[C@@]12C=CCN3[C@@H]1[C@]4(CC3)[C@H]([C@]([C@@H]2OC(=O)C)(C(=O)OC)O)N(C5=CC(=C(C=C45)[C@]6(C[C@@H]7C[C@H](CN(C7)CC8=C6NC9=CC=CC=C89)C(C)(F)F)C(=O)OC)OC)C.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
YIHUEPHBPPAAHH-IIQAEXPMSA-N
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| InChi Code |
InChI=1S/C45H54F2N4O8.2C4H6O6/c1-8-42-14-11-16-51-17-15-43(36(42)51)30-19-31(34(56-5)20-33(30)49(4)37(43)45(55,40(54)58-7)38(42)59-25(2)52)44(39(53)57-6)21-26-18-27(41(3,46)47)23-50(22-26)24-29-28-12-9-10-13-32(28)48-35(29)44;2*5-1(3(7)8)2(6)4(9)10/h9-14,19-20,26-27,36-38,48,55H,8,15-18,21-24H2,1-7H3;2*1-2,5-6H,(H,7,8)(H,9,10)/t26-,27+,36-,37+,38+,42+,43+,44-,45-;2*1-,2-/m011/s1
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| Chemical Name |
(2R,3R)-2,3-dihydroxybutanedioic acid;methyl (1R,9R,10S,11R,12R,19R)-11-acetyloxy-4-[(12S,14S,16R)-16-(1,1-difluoroethyl)-12-methoxycarbonyl-1,10-diazatetracyclo[12.3.1.03,11.04,9]octadeca-3(11),4,6,8-tetraen-12-yl]-12-ethyl-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
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
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| 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.
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.
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