A selective IDO1 inhibitor (IC50s = 67 and 19 nM for human IDO in enzymatic activity and HeLa cell assays

INCB024360 analog – 5 mg

Brand:
Cayman
CAS:
914471-09-3
Storage:
-20
UN-No:
Non-Hazardous - /

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.{29738,30726,30725} It is inactive against tryptophan 2,3-dioxygenase (IC50 > 10 µM).{30726} 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.{30726} A fluorine-18 moiety has been used to label this compound for use as a probe for imaging IDO1 expression via positron emission tomography.{30724}  

 

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Description

A selective IDO1 inhibitor (IC50s = 67 and 19 nM for human IDO in enzymatic activity and HeLa cell assays, respectively); decreases kynurenine levels in plasma and dose-dependently reduces the growth of GM-CSF-secreting B16 tumor xenografts in mice at 25-75 mg/kg

Formal name: 4-amino-N’-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide

Synonyms:  IDO5L

Molecular weight: 271.6

CAS: 914471-09-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Amino Acid Turnover||Research Area|Cancer

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