JBJ-09-063 TFA

JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC 50 s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR , Akt and ERK1/2 ph Appearance:Solid IC50& Target:EGFR L858R 0.147 nM (IC 50 ) EGFR L858R/T790M 0.063 nM (IC 50 ) EGFR L858R/T790M/C797S 0.083 nM (IC 50 ) EGFRLT/L747S 0.396 nM (IC 50 ) In Vitro:JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation. JBJ-09-063 is effective in In Vivo:JBJ-09-063 (3mg/kg i.v., 20mg/kg p.o.) exhibits favorable pharmacokinetics properties and is sufficiently stable to deliver good efficacy upon oral dosing. MCE has not independently confirmed the accuracy of these methods. They are for reference on Biological Activity:JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC 50 s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR , Akt and ERK1/2 ph

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