JBJ-04-125-02 

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 0.26 nM for EGFR^L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR^{L858R/T790M/C797S} signaling. JBJ-04-125-02 has anti-tumor activities^[1].

JBJ-04-125-02 (0-1000 nM; 72 hours; H1975 cells) treatment could inhibit cell proliferation of H1975 cells at low nanomolar concentrations^[1].
JBJ-04-125-02 treatment also inhibits cell proliferation in Ba/F3 cells stably transfected with EGFR^L858R, EGFR^L858R/T790M, or EGFR^{L858R/T790M/C797S} mutations^[1].
The ability of JBJ-04-125-02 (0.01-10 μM) to inhibit EGFR phosphorylation using Ba/F3, H1975 and NIH-3T3 cells is examined. JBJ-04-125-02 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JBJ-04-125-02 (50 mg/kg; oral gavage; once daily; for 15 weeks; EGFR^{L858R/T790M/C797S} genetically engineered mice) treatment leads to marked tumor regressions within 4 weeks of treatment^[1].
JBJ-04-125-02 exhibits a moderate half-life of 3 hours and a high area under curve of 728,577 min•ng/mL (AUClast) following 3 mg/kg intravenous (i.v.) dose. A 20 mg/kg oral dose of JBJ-04-125-02 achieves an average maximal plasma concentration of 1.1 μmol/L with an oral bioavailability of 3%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

543.61

C₂₉H₂₆FN₅O₃S

2060610-53-7

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Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. To C, et al. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943.  [Content Brief]