Cas No.: | 914471-09-3 |
Chemical Name: | INCB14943 |
Synonyms: | INCB024360;INCB024360 analogue;4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3 -carboximidamide;IDO-IN2;IDO-IN-2;INCB-24360;IDO5L;4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide;INCB 024360-analog;4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboxamidine;2HR315841W;IDO inhibitor 5l;INCB14943;AOB6408;HGXSLPIXNPASGZ-UHFFFAOYSA-N;HMS3653H15;BDBM347045;BCP08453;US10202388, Ref. B;s7587;ABP00 |
SMILES: | ClC1=C(C([H])=C([H])C(=C1[H])/N=C(/C1C(N([H])[H])=NON=1)\N([H])O[H])F |
Formula: | C9H7ClFN5O2 |
M.Wt: | 271.63 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | IDO5L is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 67 nM. |
In Vivo: | Testing of IDO5L in mice demonstrates pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors. Initial oral pharmacokinetic studies show that IDO5L is rapidly cleared (t1/2<0.5 h) and that oral administration will not be a suitable dosing method for in vivo studies. The measured plasma exposure (2.5 μM) of IDO5L during this period exceeded our calculated mouse protein binding adjusted B16 cellular IC50 (PBadjIC50=1.0 μM, murine cellular B16 IC50=46 nM). Notably, kynurenine levels increase back to baseline after 4 h as IDO5L exposure levels decreased below the mouse PBadjIC50 from 1.0 to 0.1 μM[1]. |
In Vitro: | IDO5L (Compound 5l) is a potent (HeLa IC50=19 nM) inhibitor of IDO[1]. IDO5L is one of the highest potent inhibitors of the IDO1 (IC50=19 nM, in HeLa cell assay)[2]. |