ALK-IN-12

ALK-IN-12 is a potent and orally active ALK inhibitor with an IC₅₀ of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC₅₀=20.3 and 90.6 nM). Antitumor activities^[1]. In Vitro: ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC₅₀ of 28.3 nM^[1]. In Vivo: ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity^[1].
ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC_0-∞, CL, t_1/2 and V_ss are 3039 ng?h/mL, 0.91 h?kg, 6.6 hours and 6.12 L/kg, respectively^[1].
ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows C_max, AUC_0-∞, t_max, t_1/2 and F are 3254 ng/mL, 4056 ng?h/mL, 6.0 hours, 12.5 hours and 39%, respectively^[1].