Vincristine (NSC-67574) sulfate

Catalog No.S1241 Synonyms: Leurocristine, Oncovin, 22-Oxovincaleukoblastine

For research use only.

Vincristine sulfate (NSC-67574, Leurocristine, Oncovin, 22-Oxovincaleukoblastine) 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.

Vincristine (NSC-67574) sulfate Chemical Structure

CAS No. 2068-78-2

Selleck's Vincristine (NSC-67574) sulfate has been cited by 101 publications

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

Biological Activity

Description Vincristine sulfate (NSC-67574, Leurocristine, Oncovin, 22-Oxovincaleukoblastine) 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.
Targets
Microtubules [1]
(Cell-free assay)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Melanoma cells NVS0VYtYS3m2b4TvfIlkcXS7IHHzd4F6 MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDt[Yxidm:vYTDj[YxteyxiR1m1NEA:KDBwMUW4OFkh|ryPLh?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDV7OECxPEc,OTh3OUiwNVg9N2F-
Melanoma cells M4D4NGFvfGm2dX3vdkBie3OjeR?= NXHWcWRsSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdWWuYX7vcYEh[2WubIOsJGdKPTBiPTCwMlE2QDR7IN88UU4> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV3OUKwOUc,OTd3NUmyNFU9N2F-
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Melanoma cells MXzDfZRwfG:6aXPpeJkh[XO|YYm= MVG0PEBpenN? NXrPVmZjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdWWuYX7vcYEh[2WubIOgZYZ1\XJiNEigbJJ{NCCJSUWwJF0hOC5zNjFOwG0v NYjs[5dsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyPFM1OzBpPkKyNlg{PDNyPD;hQi=>
A549 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NV\1UXdmPDhiaILz M4K5ZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD6xO|E2KM7:TT6= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB|OEOyN{c,OjhyM{izNlM9N2F-
NSCLC MlHvRY51cXS3bX;yJIF{e2G7 M4Hz[lQ5KGi{cx?= NGq5NpVCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOV2NNSyClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUSB;IECuNlUh|ryPLh?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTByNkK4OUc,OTlyME[yPFU9N2F-
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NSCLC MYrDfZRwfG:6aXPpeJkh[XO|YYm= M{XBWlQ5KGi{cx?= MnjDR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUnNEVENiY3XscJMh[W[2ZYKgOFghcHK|LDDHTVUxKD1iMD6yOUDPxE1w NGTvfYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4N|Q{OCd-MkKyPFM1OzB:L3G+
NSCLC MmnIR5l1d3SxeHnjbZR6KGG|c3H5 MmPOOFghcHK| MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOV2NNSyClZXzsd{Bi\nSncjC0PEBpenNuIFfJOVAhRSByLkK1JO69VS5? M{m1V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{S3O|Q6Lz5{NEe0O|c1QTxxYU6=
NSCLC NH\LV29CdnSrdIXtc5Ih[XO|YYm= NWHSNGx7SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhVlOFTFOgZ4VtdHNuIFfJOVAhRSByLkK1NVE6KM7:TT6= NVnMb2tTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1OVkzODVpPkG3OVU6OjB3PD;hQi=>
NSCLC NWCxXFF{SW62aYT1cY9zKGG|c3H5 MYS0PEBpenN? M1mwRWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7TR2xEKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTBiPTCwMlI2OTF7IN88UU4> NVH3boRWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmwNFYzQDVpPkG5NFA3Ojh3PD;hQi=>
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breast cancer cells M1PYemFvfGm2dX3vdkBie3OjeR?= NIjFVGE1QCCqcoO= Mnm3RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQoLlZZN1KGOjbnPldkBk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxKD1iMD6zNVYzOyEQvF2u NYH1RodURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmwNFYzQDVpPkG5NFA3Ojh3PD;hQi=>
renal cancer cells MVzBcpRqfHWvb4KgZZN{[Xl? M2DwOWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JJJmdmGuIIT1cY9zKGOnbHzzMEBIUTVyIE2gNE4{OTZ{MzFOwG0v M2fFZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUW5NlA2Lz5zN{W1PVIxPTxxYU6=
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Assay
Methods Test Index PMID
Western blot MPM2 / Cyclin B1 / Cdc25c / p-Cdc2 / Cdc2 / Aurora B / p-H3 / p-PLK1 26156322
Growth inhibition assay Cell viability 26156322
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]

Protocol (from reference)

Cell Research:[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 Research:[6]
  • Animal Models: Human rhabdomyosarcoma xenografts Rh12
  • Dosages: 3 mg/kg
  • Administration: A single i.p. administration

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 923.04
Formula

C46H58N4O14S

CAS No. 2068-78-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C=O)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04448834 Suspended Drug: Blinatumomab B-cell Acute Lymphoblastic Leukemia Dorothy Sipkins MD PhD|Amgen|Acrotech Biopharma LLC|Duke University May 24 2021 Phase 2
NCT03981510 Recruiting Diagnostic Test: 3D-Transit Constipation|Childhood Acute Lymphoblastic Leukemia|Neurofibromatosis 1|Chronic Constipation With Overflow University of Aarhus June 13 2019 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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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.

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