K 858

Catalog No.S5933 Batch:S593301

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Technical Data

Formula

C13H15N3O2S

Molecular Weight 277.34 CAS No. 72926-24-0
Solubility (25°C)* In vitro DMSO 55 mg/mL (198.31 mM)
Ethanol 4 mg/mL (14.42 mM)
Water 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.)

Preparing Stock Solutions

Biological Activity

Description K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily.
Targets
Eg5 [1]
1.3 μM
In vitro K858 blocked centrosome separation, activated the spindle checkpoint, and induced mitotic arrest in cells accompanied by the formation of monopolar spindles. Long-term continuous treatment of cancer cells with K858 resulted in antiproliferative effects through the induction of mitotic cell death, and polyploidization followed by senescence. In contrast, treatment of nontransformed cells with K858 resulted in mitotic slippage without cell death, and cell cycle arrest in G1 phase in a tetraploid state. K858 has minimal effects on abnormalities in the number and structure of chromosomes. K858 has no effect on microtubule polymerization in cell-free and cell-based assays[1].
In vivo K858 exhibits potent antitumor activity in xenograft models of cancer, and induces the accumulation of mitotic cells with monopolar spindles in tumor tissues. K858 is not neurotoxic in a motor coordination test in mice[1].

Protocol (from reference)

Cell Assay:

[1]

  • Cell lines

    HCT116 cells

  • Concentrations

    3 μM

  • Incubation Time

    18 h

  • Method

    HCT116 cells are treated with vehicle, paclitaxel, vincristine, K858, or monastrol for 18 h.

Animal Study:

[1]

  • Animal Models

    BALB/cAJcl-nu mice inoculated with A2780 cells

  • Dosages

    150 and 50 mg/kg

  • Administration

    oral

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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.