| Identification | Back Directory | [Name]
Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]- | [CAS]
1923844-48-7 | [Synonyms]
BMS-986242
Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]- | [Molecular Formula]
C24H24ClFN2O | [MDL Number]
MFCD34474214 | [MOL File]
1923844-48-7.mol | [Molecular Weight]
410.91 |
| Chemical Properties | Back Directory | [Boiling point ]
593.0±40.0 °C(Predicted) | [density ]
1.228±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (608.41 mM; Need ultrasonic) | [form ]
Solid | [pka]
14.09±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
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[1].
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)[1].
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[1]. | [References]
[1]. Cherney EC, et al. Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1. ACS Med Chem Lett. 2021;12(2):288-294. Published 2021 Jan 28. |
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