JBJ-09-063 - CAS 2820336-67-0

JBJ-09-063 is a mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR), with potent inhibitory activity demonstrated by half-maximal inhibitory concentrations (IC50s) of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. This compound effectively decreases phosphorylation of EGFR, Akt, and ERK1/2, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI) -sensitive and resistant models. JBJ-09-063 holds potential for research into EGFR-mutant lung cancer.

Others, EGFR

Others, Tyrosine Kinase/Adaptors, Angiogenesis, JAK/STAT signaling

2820269

C31H29FN4O3S

556.65

C(C(NC1=NC=CS1)=O)(N2C(=O)C=3C(C2)=CC=C(C3)C4=CC=C(C=C4)C5CCN(C)CC5)C6=C(O)C=CC(F)=C6

-20°C

Ice Packs

Small Compound