Antibodies
Vincristine
- 貨號 Cat. No.
- S1241
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Vincristine
Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Vincristine is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM. | |||||
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| Targets | Microtubules | |||||
| IC50 | 32 μM [1] | |||||
| 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] | |||||
| Features | ||||||
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 |
|---|---|
| Dosages | 3 mg/kg |
| Administration | A single i.p. administration |
| Solubility | Saline, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01946529 | Recruiting | Desmoplastic Small Round Cell Tumor|Ewing Sarcoma of Bone|Localized Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor | St. Jude Children’s Research Hospital | 2013-11 | Phase 2 |
| NCT02017964 | Not yet recruiting | Untreated Childhood Medulloblastoma | Children’s Oncology Group|National Cancer Institute (NCI) | 2013-12 | Phase 2 |
| NCT01974440 | Not yet recruiting | Lymphoma | Janssen Research & Development, LLC|Pharmacyclics | 2014-01 | Phase 3 |
| NCT01775475 | Not yet recruiting | AIDS-related Diffuse Large Cell Lymphoma|AIDS-related Diffuse Mixed Cell Lymphoma|AIDS-related Diffuse Small Cleaved Cell Lymphoma|AIDS-related Immunoblastic Large Cell Lymphoma|AIDS-related Lymphobla | AIDS Malignancy Clinical Trials Consortium|National Cancer Institute (NCI) | 2014-01 | Phase 2 |
| NCT01539174 | Not yet recruiting | Contiguous Stage II Adult Diffuse Large Cell Lymphoma|Noncontiguous Stage II Adult Diffuse Large Cell Lymphoma|Stage I Adult Diffuse Large Cell Lymphoma|Stage III Adult Diffuse Large Cell Lymphoma|Sta | Fox Chase Cancer Center|Genentech | 2014-03 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 923.04 |
|---|---|
| Formula | C46H58N4O14S |
| CAS No. | 2068-78-2 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | leurocristine, Oncovin |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (108 mM) |
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| Water | 60 mg/mL (65 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | Saline, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.92304 | 9.2304 | 18.4608 | 27.6912 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| 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 (2)
Targeting Sonic Hedgehog-Associated Medulloblastoma through Inhibition of Aurora and Polo-like Kinases. [Markant SL, et al. Cancer Res 2013;73(20):6310-22]
Combined Treatment with an Oncolytic Adenovirus and Antitumor Activity of Vincristine against Retinoblastoma Cells. [Song X, et al. Int J Mol Sci 2012;13(9):10736-49]
