INCB024360 analog

Indoleamine 2,3-dioxygenase (IDO) metabolizes tryptophan to kynurenine, leading to the production of NAD+ via the kynurenine pathway. It has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. INCB024360 analog is a potent IDO1 inhibitor that demonstrates IC50 values of 67 and 19 nM for human IDO in enzymatic activity and HeLa cell assays, respectively. It is inactive against tryptophan 2,3-dioxygenase (IC50 > 10 µM). At 25-75 mg/kg, subcutaneous administration of INCB024360 analog to mice significantly decreased kynurenine levels in plasma and dose-dependently reduced the growth of GM-CSF-secreting B16 tumor xenografts. A fluorine-18 moiety has been used to label this compound for use as a probe for imaging IDO1 expression via positron emission tomography.Formal Name: 4-amino-N'-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide. CAS Number: 914471-09-3. Synonyms: IDO5L. Molecular Formula: C9H7ClFN5O2. Formula Weight: 271.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, Ethanol: 30 mg/mL, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/mL. lambdamax: 246, 285 nm. SMILES: ON/C(C1=NON=C1N)=N\C2=CC=C(F)C(Cl)=C2. InChi Code: InChI=1S/C9H7ClFN5O2/c10-5-3-4(1-2-6(5)11)13-9(14-17)7-8(12)16-18-15-7/h1-3,17H,(H2,12,16)(H,13,14). InChi Key: HGXSLPIXNPASGZ-UHFFFAOYSA-N.