Home Apoptosis p53 activator COTI-2 For research use only.

COTI-2

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

COTI-2 Chemical Structure

CAS No. 1039455-84-9

Purity & Quality Control

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

COTI-2 Related Products

Signaling Pathway

p53 Signaling Pathways

p53 Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models NCr-nu mice
Dosages 10 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 366.48 Formula

C19H22N6S
CAS No. 1039455-84-9 SDF Download COTI-2 SDF
Smiles C1CC2=C(C(=NNC(=S)N3CCN(CC3)C4=CC=CC=N4)C1)N=CC=C2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6.25 mg/mL ( (17.05 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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