Biological Activity
| Description |
Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM. |
| Targets |
Microtubules |
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| IC50 |
32 μM [1] |
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| In vitro |
Vincristine inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with Ki of 85 nM. [1] At low concentrations, Vincristine stabilizes the spindle apparatus resulting in failure of the chromosomes to segregate leading to metaphase arrest and inhibition of mitosis. At higher concentrations, Vincristine may disrupt and induce total depolymerization of microtubules. [2] Vincristine induces apoptosis in tumor cells and inhibits SH-SY5Y cell proliferation with IC50 of 0.1 µM. Vincristine induces mitotic arrest and promots the expression of caspase-3 and -9 and cyclin B, while decreasing the expression of cyclin D. [4] Vincristine induced neurotoxicity is caused by interference with microtubule function, which results in blockage of axonal transport and thus in axonal degeneration. [5] |
| In vivo |
Vincristine (3 mg/kg) administrated by a single i.p. injection to mice bearing bilateral subcutaneous xenografts Rh12 or Rh18, induces mean growth delay of >120 and >52 day, and repopulating fractions of 0.06% and 5%, respectively. [6] Vincristine acts on subcutaneous colon 38 tumors in mice by host cell-mediated vascular effects as well as by direct tubulin-mediated cytotoxicity. Vincristine (5 mg/kg) reduces tumor blood flow of tumors by nearly 75% . [7] |
| Clinical Trials |
Phase II study on the safety and efficacy of Vincristine in relapsed acute lymphoblastic leukemia has been completed. |
| Features |
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Protocol(Only for Reference)
Cell Assay: [1]
| Cell lines |
B16 melanoma cell |
| Concentrations |
10 nM |
| Incubation Time |
3 days |
| Method |
Cells are plated in 2 mL of medium in 35-mm plates at a concentration of about 5 × 104 cells/mL and grow for 24 h at 37 ℃ in an atmosphere of 5% CO2 and 95% air. Then medium is replaced with fresh medium lacking or containing 4 nM drug and proliferation is continued for 3 days. Cell counts are done each day in a Coulter Counter after detaching the cells with trypsin and EDTA. |
Animal Study: [6]
| Animal Models |
Human rhabdomyosarcoma xenografts Rh12 |
| Formulation |
Water solutioin |
| Dosages |
3 mg/kg |
| Administration |
A single i.p. administration |
1
References
[1] Jordan MA, et al. Cancer Res, 1985, 45(6), 2741-2747.
[2] Gidding CE. Crit Rev Oncol Hematol, 1999, 29(3), 267-287.
[3] Takano Y, et al. Pathol Res Pract, 1993, 189(2), 197-203
[4] Tu Y, et al. Int J Mol Med, 2013, 31(1), 113-119.
[5] Donoso JA, et al. Cancer Res, 1977, 37(5), 1401-1407.
[6] Horton JK, et al. Biochem Pharmacol, 1988, 37(20), 3995-4000.
[7] Baguley BC, et al. Eur J Cancer, 1991, 27(4), 482-487.
Download Vincristine SDF
| Molecular Weight (MW) |
923.04 |
| Formula |
C46H58N4O14S
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| CAS No. |
2068-78-2 |
| Synonyms |
leurocristine, Oncovin |
Solubility (25°C)
- DMSO 100 mg/mL
- Water 60 mg/mL
- Ethanol <1 mg/mL
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| Storage |
2 years -20°CPowder |
| 2 weeks4°Cin DMSO |
| 6 months-80°Cin DMSO |
Research Area
Customer Reviews (1)
Click to enlarge
for HXO-RB44 cells, IC50 values for VCR were changed in the different SG600 treatment groups. The results are representative of three independent experiments and of f our replicates in each experiment.
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Rating |
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| Source |
Int J Mol Sci, 2012, 13(9), 10736-10749 . Vincristine purchased from Selleck |
| Method |
Cell Viability Assay |
| Cell Lines |
HXO-RB44 cells |
| Concentrations |
0.1-100 nM |
| Incubation Time |
96 h |
| Results |
Compared with the treatment with SG600 or VCR alone, the survival rates of RB cells decreased markedly when treated with the combination of SG600 and VCR in the process with increasing dose. Cytotoxicity of VCR in the HXO-RB44 cell line was also evaluated by IC50 values (Figure B). |
Product Citations (1)
Tech Support & FAQs
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)
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