LDC8201

LDC8201 (14 nM to 30 μM; 72 h) potently inhibits cell viability in EGFR^{H773_V774insNPH} and Her2^{A775_G776insYVMA} Ba/F3 cells (GI₅₀ = 48 nM and 59 nM, respectively), EGFR^{V769_D770insASV} Cuto 14 cells (GI₅₀ = 39 nM), and EGFR^{H773_V774insNPH} Cuto 17 cells (GI₅₀ = 23 nM), with moderate selectivity (6-fold) over EGFR wild-type A431 cells (GI₅₀ = 303 nM)^[1].
LDC8201 exhibits moderate in vitro ADME properties, including moderate microsomal and hepatocyte clearance, high plasma protein binding, moderate Caco-2 permeability, low hERG inhibition, and low cytotoxicity in normal cells^[1].
LDC8201 (8 decreasing concentrations; 72 h) potently inhibits the growth of Ba/F3-EGFR-H773_V774insNPH cells with a GI₅₀ of 48 nM and an EC₅₀ of 53 nM^[2].
LDC8201 (8 decreasing concentrations; 72 h) potently inhibits the growth of Ba/F3-Her2^{A775_G776insYVMA} cells with a GI₅₀ of 59 nM and an EC₅₀ of 86 nM^[2].
LDC8201 (8 decreasing concentrations; 72 h) potently inhibits the growth of H1975 cells with a GI₅₀ of 18 nM^[2].
LDC8201 (0.01-1 μM) inhibits EGFR activation and downstream ERK signaling in Cuto 17 cells at concentrations as low as 10 nM^[2].
LDC8201 (0.01-1 μM) inhibits EGFR activation and downstream ERK signaling in A431 cells at concentrations of 100 nM and above, demonstrating wild-type-sparing activity^[2].
LDC8201 (1 μM) has moderate metabolic stability in mouse liver microsomes with an intrinsic clearance of 93 μL/min/mg^[2].
LDC8201 (10 μM; 2 h) has moderate permeability across Caco-2 cell monolayers with an apical-to-basolateral P_app of 51 nm/s^[2].

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