COTI-2

Catalog No.S8580 Batch:S858001

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Technical Data

Formula

C19H22N6S
Molecular Weight 366.48 CAS No. 1039455-84-9
Solubility (25°C)* In vitro DMSO 6.25 mg/mL (17.05 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:

[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 Study:

[2]
  • Animal Models

    NCr-nu mice

  • Dosages

    10 mg/kg

  • Administration

    i.p.

Selleck's COTI-2 has been cited by 2 publications

The combination of breast cancer PDO and mini-PDX platform for drug screening and individualized treatment [ J Cell Mol Med, 2024, 28(9):e18374] PubMed: 38722288
Generation of an Isogenic Cell Line Model to Test Novel Treatment Options for TP53-Mutant AML [ DASH, 2020, None] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.