(Rac)-JBJ-04-125-02

Catalog No.S8920 Synonyms: JBJ-04-125-02 racemate

For research use only.

(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.

(Rac)-JBJ-04-125-02 Chemical Structure

CAS No. 2140807-05-0

Purity & Quality Control

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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 Research:

[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. For experiments that investigate the effect of JBJ-04-125-02 in the presence of EGF or cetuximab, 10ng/ml of EGF, 1μg/ml or 10μg/ml of cetuximab added at the same time that cells are treated with inhibitors.

Animal Research:

[1]

  • Animal Models: male C57Bl/6 mice
  • Dosages: 50 mg/kg, 100 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(183.95 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 543.61
Formula

C29H26FN5O3S

CAS No. 2140807-05-0
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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