COTI-2

Catalog No.S8580

For research use only.

COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.

COTI-2 Chemical Structure

CAS No. 1039455-84-9

Selleck's COTI-2 has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.
Targets
p53 mutants [1]
()
In vitro

The thiosemicarbazone COTI-2 is reported to promote refolding of mutant p53 and restore wild-type-p53 function. It is active against human tumour cell lines of various origins at nanomolar concentrations, induces cell death by apoptosis[1]. COTI-2 is highly efficacious against multiple cancer cell lines from a broad range of human cancers both in vitro and in vivo. COTI-2 does not significantly inhibit over 200 kinases from major kinase pathways involved in cancer that were evaluated in both kinase assays and does not inhibit the ATPase activity of Hsp90, a ubiquitous molecular chaperone that plays an essential role in cell survival and cell cycle control[2].

In vivo COTI-2 significantly inhibited tumor growth in the HT-29 human colorectal tumor xenografts at a dose of 10 mg/kg. COTI-2 also significantly inhibited tumor growth in the SHP-77 SCLC xenograft model at a dose as low as 3 mg/kg. Its treatment delays U87-MG, MDA-MB-231 and OVCAR-3 xenograft growth. COTI-2 treatment demonstrates a safe toxicity profile in vivo. COTI-2 selectively targets a wide variety of human cancer cell lines, as demonstrated by the in vitro data, while having little deleterious effects on normal cells[2].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: SHP-77 cells
  • Concentrations: 100, 250, 1000 nM
  • Incubation Time: 48 h
  • Method:

    SHP-77 cells were cultured with various concentrations of COTI-2 for 48 h. Cells were then washed twice with 1X cold PBS and stained with Annexin V and 7AAD. Briefly, 5 μl of Annexin V and 7AAD were added to 1 × 105 cells and incubated for 15 min at room temperature in the dark. Then 400 μl of the 1X binding buffer was added to the cells.

Animal Research:

[2]

  • Animal Models: NCr-nu mice
  • Dosages: 10 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 73 mg/mL
(199.19 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 366.48
Formula

C19H22N6S

CAS No. 1039455-84-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC2=C(C(=NNC(=S)N3CCN(CC3)C4=CC=CC=N4)C1)N=CC=C2

In vivo Formulation Calculator (Clear solution)

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

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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

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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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