BMS-986242

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-986242 是一种口服有效、选择性的吲哚胺-2,3-双加氧酶 1 (IDO1) 抑制剂，可用于癌症研究。

BMS-986242 is an orally active, potent and selective inhibitor of indoleamine-2,3-dioxygenase 1 (IDO1), and it can be used for the research of cancer.

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).

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 MouseDosage: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.

BMS986242 | BMS 986242

Metabolic Enzyme/Protease

IDO

IDO1

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1923844-48-7

410.91

C24H24ClFN2O

>98% (HPLC)

DMSO:250 mg/mL (608.41 mM; Need ultrasonic)

O=C(N[C@@H]([C@H]1CC[C@@H](C2=CC=NC3=CC=C(F)C=C23)CC1)C)C4=CC=C(Cl)C=C4

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(-20℃)

With Ice Pack

≥ 2 years