Vincristine sulfate

Catalog No.S1241

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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Vincristine sulfate Chemical Structure

Vincristine sulfate Chemical Structure
Molecular Weight: 923.04

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Product Description

Biological Activity

Description Vincristine sulfate is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay.
Targets Microtubules [1]
(Cell-free assay)
IC50 32 μM
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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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JFCR39 M1fSTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mkj3NUDDvU1?M1;oU|I1KGh?MkfUSG1UVw>?MUPtZZJs\WSueTDpcoNz\WG|ZYOgeIhmKG63bXLldkBw\iCJMj;NJJBp[XOnIHPlcIx{Mn3sNlM2QTh{N{[=
A549MVjGeY5kfGmxbjDBd5NigQ>?M{nU[FExOCCwTR?=NYXDNIdXOTZiaB?=MljHSG1UVw>?NVfGOm1ydGWjZIOgeI8h[SCub4PzJI9nKG2rY4LveJVjfWyncx?=MXyyN|U6QDJ5Nh?=
SGC7901NUnWTppzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NE[4c4pKSzVyPUGuNlbjiIoEsfMAjVAvOTFizsznM41tM2LySlI{PTZ2NEiy
SGC7901/LV-NCM1XFbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYTyOGJVUUN3ME2xMlc46oDLwsJihKkxNjF4IN88[{9udA>?M1KxWFI{PTZ2NEiy
SGC7901/LV-SGO1MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUjV[5FTUUN3ME20MlM36oDLwsJihKkxNjN5IN88[{9udA>?M4nNTFI{PTZ2NEiy
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SGC7901/VCR-NCNUnrU4dMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NGX2XHdKSzVyPUG5Mlg36oDLwsJihKkzNjBzIN88[{9udA>?MoXJNlM2PjR2OEK=
SGC7901/VCR-si-SGO1M4XqUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHrxN4VKSzVyPU[uNVjjiIoEsfMAjVEvODNizsznM41tMYWyN|U3PDR6Mh?=
SGC7901/ADRM{HDTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVfJR|UxRTdwOEZihKnDueLCiUCuOlQh|rypL33sMX[yN|U3PDR6Mh?=
SGC7901/ADR-NCM2XCSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVzJR|UxRThwOURihKnDueLCiUCuOlgh|rypL33sM1vXU|I{PTZ2NEiy
SGC7901/ADR-si-SGO1M{jXVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3fZU2lEPTB;Mz60OwKBkcLz4pEJNE4zQSEQvHevcYw>MlXNNlM2PjR2OEK=
SH-SY5Y M3rQS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHG0PI8xNjByMT2xNEDPxE1?M{PpcVI1KGh?MWPJR|UxRTBwMUGzxtExNjBzMjFOwG0>M2S3UVI{OTJ7ME[1
SH-SY5Y MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M33FRVAvODBzLUGwJO69VQ>?NGTjRZk1QCCqMWLJR|UxRTBwMEe4xtExNjByOTFOwG0>NUDFPIRJOjNzMkmwOlU>
SH-SY5Y M3PWPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnG0NE4xODFvMUCg{txOM2m3eVczKGh?MmLOTWM2OD1yLkC1NeKyOC5yMEig{txONVTZeGtEOjNzMkmwOlU>
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... Click to View More Cell Line Experimental Data

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
Formulation Water solutioin
Dosages 3 mg/kg
Administration A single i.p. administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
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.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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 Imm  ...more 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  ...more 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  ...more 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

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Chemical Information

Download Vincristine sulfate SDF
Molecular Weight (MW) 923.04
Formula

C46H58N4O14S

CAS No. 2068-78-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms Leurocristine
Solubility (25°C) * In vitro DMSO 100 mg/mL (108.33 mM)
Water 60 mg/mL (65.0 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.
Chemical Name  22-​oxo-vincaleukoblastine, sulfate (1:1)

Frequently Asked Questions

  • Question 1
    I want to use the product #S1421 for mouse in vivo, could you please give us your advice about administration method?

    Answer: 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.

Tech Support

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.

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