JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally activeEGFRinhibitor with anIC₅₀of 0.26 nM forEGFR^L858R/T790M. JBJ-04-125-02 can inhibitcancercell proliferation andEGFR^{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].

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 minong/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].

543.61

C₂₉H₂₆FN₅O₃S

2060610-53-7

Room temperature in continental US; may vary elsewhere.

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