货号:A165598 同义名: INCB024360 analog;Epacadostat analogue
INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.
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描述 | IDO5L is a potent inhibitor of IDO with an IC50 value of 19 nM in Hela cells[1]. |
体内研究 | Evaluation of IDO5L in mice illustrates pharmacodynamic inhibition of IDO, as evidenced by decreased kynurenine levels (>50%) in plasma and dose-dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors. Initial oral pharmacokinetic studies reveal rapid clearance of IDO5L (t1/2<0.5 h), rendering oral administration unsuitable for in vivo studies. Plasma exposure measurements (2.5 μM) of IDO5L during this period surpass the calculated mouse protein binding-adjusted B16 cellular IC50 (PBadjIC50=1.0 μM, murine cellular B16 IC50=46 nM). Notably, kynurenine levels return to baseline after 4 hours as IDO5L exposure levels drop below the mouse PBadjIC50 from 1.0 to 0.1 μM[1]. |
体外研究 | IDO5L is a potent inhibitor of IDO with an IC50 value of 19 nM in Hela cells[1]. |
作用机制 | INCB024360 Analogue is a reversible and competitive inhibitor of IDO1, which can bound to IDO through the oxygen of the hydroxyamidine to the iron of the heme in the ferrous state. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
HEK293 clone 6 cells | Function assay | Inhibition of human IDO1 transfected in HEK293 clone 6 cells by HPLC analysis | 22616902 | ||
human HeLa cells | Function assay | Inhibition of indoleamine 2,3-dioxygenase in IFN-gamma-stimulated human HeLa cells assessed as kynurenine formation by spectrophotometry, IC50=19 nM | 19507862 | ||
mouse B16 cells | Function assay | Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by spectrophotometry, IC50=46 nM | 19507862 | ||
mouse P815B clone-6 cells | Function assay | Inhibition of human IDO1 transfected in mouse P815B clone-6 cells by HPLC analysis, IC50=60 nM | 22616902 | ||
Dose | Mice: min = 25 mg/kg, max = 100 mg/kg (s.c.) 25 mg/kg - 100 mg/kg (p.o.) |
Administration | s.c., p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.68mL 0.74mL 0.37mL |
18.41mL 3.68mL 1.84mL |
36.81mL 7.36mL 3.68mL |
CAS号 | 914471-09-3 |
分子式 | C9H7ClFN5O2 |
分子量 | 271.636 |
别名 | INCB024360 analog;Epacadostat analogue;INCB14943 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(184.07 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear PO 0.5% CMC-Na 30 mg/mL suspension |