Home Apoptosis p53 activator COTI-2

research use only

COTI-2 p53 activator

Cat.No.S8580

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

Chemical Structure

Molecular Weight: 366.48

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S858001 DMSO]6.25 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.51%
99.51

Chemical Information, Storage & Stability

Molecular Weight 366.48 Formula

C19H22N6S

 Storage (From the date of receipt)
CAS No. 1039455-84-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CC2=C(C(=NNC(=S)N3CCN(CC3)C4=CC=CC=N4)C1)N=CC=C2

Solubility

In vitro
Batch:

DMSO : 6.25 mg/mL (17.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% 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.

Mechanism of Action

Targets/IC50/Ki
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]. This compound is highly efficacious against multiple cancer cell lines from a broad range of human cancers both in vitro and in vivo. It 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. This compound 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. This chemical treatment demonstrates a safe toxicity profile in vivo. It 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].
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map