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INCB 024360-analog
- IDO inhibitor 5l
- Soluble in DMSO
- MF: C9H7ClFN5O2
- MW: 271.64
Description
Potent competitive inhibitor of indoleamine 2,3-dioxygenase (IDO1, IC50 value 67 nM) with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model; This INCB024360-analog decreased kynurenine levels by >50% in plasma and inhibited B16-GM-CSF tumor growth in a dose dependent fashion.
INCB 024360 (or Epacadostat; Axon 1733) is available from Axon Medchem as well.
More Information
| Parent CAS No. | 914471-09-3 |
|---|---|
| Chemical Name | 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide |
| SMILES | C1C=C(F)C(Cl)=CC=1NC(=NO)C1C(N)=NON=1 |
| MFCD | MFCD18633286 |
| InChi | 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) |
| InChiKey | HGXSLPIXNPASGZ-UHFFFAOYSA-N |
| CID | 135424953 |
| Short Description | IDO1 inhibitor |
References
- E.W. Yue et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J. Med. Chem. 2009, 52, 7364-7367.
- X. Liu et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood 2010, 115, 3520-3530.
- X. Huang et al. Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression. J Labelled Comp Radiopharm. 2015 Apr;58(4):156-62.
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