Catalog No.S1241 Synonyms: Leurocristine
Molecular Weight(MW): 923.04
Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay.
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Plk inhibitor cooperates with chemotherapeutic agents. Conditional patched mutant tumor cells were treated with increasing concentrations of the chemotherapeutic agents vincristine alone or in combination with 10 nMol/L BI-2536. Cells were cultured for 48 hours, pulsed with 3H-Td, and harvested for analysis of 3H-Td incorporation at 66 hours.
Cancer Research, 2013, 73(20): 6310-22 . Vincristine sulfate purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|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 inhibits net addition of tubulin dimers at assembly ends of steady-state microtubules with Ki of 85 nM.  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.  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.  Vincristine induced neurotoxicity is caused by interference with microtubule function, which results in blockage of axonal transport and thus in axonal degeneration. 
|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.  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% . |
-  Jordan MA, et al. Cancer Res, 1985, 45(6), 2741-2747.
-  Gidding CE. Crit Rev Oncol Hematol, 1999, 29(3), 267-287.
-  Tu Y, et al. Int J Mol Med, 2013, 31(1), 113-119.
|In vitro||DMSO||100 mg/mL (108.33 mM)|
|Water||60 mg/mL (65.0 mM)|
|In vivo||Saline||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02828358||Not yet recruiting||Acute Leukemia of Ambiguous Lineage|Childhood B Acute Lymphoblastic Leukemia|Mixed Phenotype Acute Leukemia||National Cancer Institute (NCI)||December 2016||--|
|NCT02724579||Not yet recruiting||Untreated Childhood Medulloblastoma||Childrens Oncology Group|National Cancer Institute (NCI)||October 2016||Phase 2|
|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 Lymphoblastic Lymphoma|AIDS-related Peripheral/Systemic Lymphoma|AIDS-related Small Noncleaved Cell Lymphoma|Stage III AIDS-related Lymphoma|Stage IV AIDS-related Lymphoma||AIDS Malignancy Consortium|National Cancer Institute (NCI)|The EMMES Corporation||September 2016||Phase 2|
|NCT02257242||Not yet recruiting||Lymphoma, Non-Hodgkin|Lymphoma, Follicular|Lymphoma, Mantle-Cell|Lymphoma, Small-Cell|Waldenstrom Macroglobulinemia|Lymphoma, B-Cell, Marginal Zone||Adam Olszewski|Spectrum Pharmaceuticals, Inc|Rhode Island Hospital|The Miriam Hospital|Brown University||September 2016||Phase 1|
|NCT02723994||Not yet recruiting||B-cell Acute Lymphoblastic Leukemia||Incyte Corporation|Childrens Oncology Group||August 2016||Phase 2|
|NCT02538926||Not yet recruiting||B Acute Lymphoblastic Leukemia|B Lymphoblastic Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent B Lymphoblastic Lymphoma|Recurrent T Lymphoblastic Leukemia/Lymphoma|Refractory B Lymphoblastic Lymphoma|Refractory T Lymphoblastic Lymphoma|T Acute Lymphoblastic Leukemia|T Lymphoblastic Lymphoma||University of Washington|National Cancer Institute (NCI)||August 2016||Phase 2|
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Frequently Asked Questions
I want to use the product #S1421 for mouse in vivo, could you please give us your advice about administration method?
According to the reference cited on our website, we test the solubility of S1421 Staurosporine in 4% DMSO/saline, and it is a suspension at 5 mg/mL. The compound can also be dissolved in the vehicle 4% DMSO/30% PEG 300/10% Tween 80/saline at 5 mg/ml as a clear solution for injection.