(Rac)-JBJ-04-125-02

Catalog No.S8920 Batch:S892001

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Technical Data

Formula

C29H26FN5O3S
Molecular Weight 543.61 CAS No. 2140807-05-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (183.95 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.)

Preparing Stock Solutions

Biological Activity

Description (Rac)-JBJ-04-125-02 (JBJ-04-125-02 racemate) is a mutant-selective allosteric inhibitor of Epidermal growth factor receptor (EGFR) with potential anticancer activity.
Targets
EGFR [1]

Biological Activity

Description (Rac)-JBJ-04-125-02 (JBJ-04-125-02 racemate) is a mutant-selective allosteric inhibitor of Epidermal growth factor receptor (EGFR) with potential anticancer activity.
Targets
EGFR [1]
In vitro

JBJ-04-125-02 can inhibit cell proliferation in vitro. Osimertinib, an ATP-competitive covalent EGFR inhibitor, uniquely and significantly enhances the binding of JBJ-04-125-02 for mutant EGFR. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, a more effective inhibition of cellular growth in vitro compared to either single agent alone.[1]
In vivo

JBJ-04-125-02 can inhibit EGFR L858R/T790M/C797S signaling in vivo. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, and an increased efficacy in vivo compared to either single agent alone.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Ba/F3, H1975, H3255GR, H3255DR cells

  • Concentrations

    0.1 nM, 1 nM, 10 nM, 0.1 μM, 1 μM

  • Incubation Time

    72 hours

  • Method

    Ba/F3, H1975, H3255GR and H3255DR cells are treated with increasing concentrations of inhibitors for 72 hours and growth or the inhibition of growth is assessed by MTS assay. 
Animal Study:

[1]
  • Animal Models

    male C57Bl/6 mice

  • Dosages

    50 mg/kg, 100 mg/kg

  • Administration

    Oral gavage

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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.