JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally activeEGFRinhibitor with anIC₅₀of 15 nM forEGFR^{L858R/T790M[1]}.

In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFR^L858R, EGFR^L858R/T790Mand EGFR^{L858R/T790M/C797S}with IC₅₀values of 9.29 μM; 8.35 μM; 8.53 μM and 2.13 μM, respectively^[1].
JBJ-02-112-05 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFR^L858R, EGFR^L858R/T790M, EGFR^{L858R/T790M/C797S}mutations^[1].

JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFR^{L858R/T790M/C797S}genetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways^[1].
JBJ-02-112-05 exhibits a moderate half-life of 3 hours and a_Cmaxof 13.7 μM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a C_Cmaxof 1.31 μM^[1].

464.54

C₂₇H₂₀N₄O₂S

2748162-29-8

Room temperature in continental US; may vary elsewhere.

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