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.
IC50&Target
IDO1
体外研究
BMS-986242 is more prone to oxidative metabolism and less susceptible to glucuronidation. BMS-986242 shows IC50>25 μM for all targets except nAChR a1 (IC50=12.3 μM) and nAChR a7 (IC50>6 μM with ∼20 % max inhibition).
体内研究
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.
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.
分子式
C24H24ClFN2O
分子量
410.91
CAS号
1923844-48-7
运输条件
Room temperature in continental US; may vary elsewhere.