JBJ-02-112-05 

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 15 nM for EGFR^{L858R/T790M[1]}.

In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFR^L858R, EGFR^L858R/T790M and EGFR^{L858R/T790M/C797S} with IC₅₀ values 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].

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

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 _Cmax of 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_Cmax of 1.31 µM^[1].

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

464.54

C₂₇H₂₀N₄O₂S

2748162-29-8

O=C(NC1=NC=CS1)C(N2C(C(C=C(C3=CC(C=CN4)=C4C=C3)C=C5)=C5C2)=O)C6=CC=CC=C6

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]