Kobe0065

Catalog No.S8303 Batch:S830301

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Technical Data

Formula

C15H11ClF3N5O4S
Molecular Weight 449.79 CAS No. 436133-68-5
Solubility (25°C)* In vitro DMSO 89 mg/mL (197.87 mM)
Ethanol 13 mg/mL (28.9 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.)

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Biological Activity

Description Kobe0065 is an H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Targets
H-Ras-cRaf1 interaction [1]
In vitro Kobe0065-family compounds bind to Ras⋅GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras⋅GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition[1].
In vivo Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    NIH 3T3 cells

  • Concentrations

    2 and 20 μM

  • Incubation Time

    1 h

  • Method

    NIH 3T3 cells are transfected with pEF-BOS-HA-H-Ras(G12V) or an empty vector and treated with the 2 and 20 μM compound or the vehicle (DMSO) in the presence of 2% FBS for 1 h. Cell lysate is subjected to detection of c-Raf-1 coimmunoprecipitated with an anti-H-Ras antibody and total c-Raf-1 by Western blotting with an anti-c-Raf-1 antibody. Immunoprecipitated H-Ras(G12V) are detected by an anti-HA antibody.
Animal Study:[1]
  • Animal Models

    A xenograft of SW480 cells in nude mice.

  • Dosages

    80 mg/kg and 160 mg/kg

  • Administration

    oral administration

Selleck's Kobe0065 has been cited by 2 publications

Glycyrrhetinic acid binds to the conserved P-loop region and interferes with the interaction of RAS-effector proteins. [ Acta Pharm Sin B, 2019, 9(2):294-303] PubMed: 30976491
RAF kinases are stabilized and required for dendritic cell differentiation and function. [ Cell Death Differ, 2019, 10.1038/s41418-019-0416-4] PubMed: 31541179

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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.