For research use only. Not for therapeutic Use.
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].
| Catalog Number | I023560 |
| CAS Number | 1923844-48-7 |
| Synonyms | 4-chloro-N-[(1R)-1-[4-(6-fluoroquinolin-4-yl)cyclohexyl]ethyl]benzamide |
| Molecular Formula | C24H24ClFN2O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H24ClFN2O/c1-15(28-24(29)18-6-8-19(25)9-7-18)16-2-4-17(5-3-16)21-12-13-27-23-11-10-20(26)14-22(21)23/h6-17H,2-5H2,1H3,(H,28,29)/t15-,16?,17?/m1/s1 |
| InChIKey | AOJCHFNHRLPISK-KLAILNCOSA-N |
| SMILES | CC(C1CCC(CC1)C2=C3C=C(C=CC3=NC=C2)F)NC(=O)C4=CC=C(C=C4)Cl |
| Reference | [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. |
