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Formula | C46H58N4O14S |
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Molecular Weight | 923.04 | CAS No. | 2068-78-2 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (108.33 mM) | |
Water | 50 mg/mL (54.16 mM) | |||
Ethanol | Insoluble | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis. | ||
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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] |
Cell Assay:[1] |
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Animal Study:[6] |
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Data from [Int J Mol Sci, 2012, 13, 10736-10749 ]
Data from [Data independently produced by , , Cancer Research, 2013, 73(20): 6310-22 ]
Data from [Data independently produced by , , Cell Death & Disease, 2017, doi:10.1038/cddis.2017.454]
Data from [Data independently produced by , , Chemosphere, 2018, 210:467-475]
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