BMS-986242 is an orally active, potent and selective indoleamine-2,3-dioxygenase 1 ( IDO1 ) inhibitor. BMS-986242 can be used for the research of cancer
In Vitro
BMS-986242 is more prone to oxidative metabolism and less susceptible to glucuronidation. BMS-986242 shows IC 50 >25 μM for all targets except nAChR a1 (IC 50 =12.3 μM) and nAChR a7 (IC 50 >6 μM with ∼20 % max inhibition). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BMS-986242 (3~30 mg/kg; p.o.; 0~24 hours) exhibits dose-proportional exposure and a statistically significant reduction in kynurenine concentration in the tumor at all three doses . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: nu/nu Mouse Dosage: 3~30 mg/kg Administration: P.o. Result: Exhibited dose-proportional exposure and a statistically significant reduction in kynurenine concentration in the tumor at all three doses.