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INCB024360 analogue
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
INCB024360 analogue图片
CAS NO:914471-09-3
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)271.64
FormulaC9H7ClFN5O2
CAS No.914471-09-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 54 mg/mL (198.8 mM)
Water: <1 mg/mL
Ethanol: 54 mg/mL (198.8 mM)
Solubility (In vivo)2% DMSO+corn oil: 5mg/mL
SynonymsIDO-IN-2;INCB024360 analog; INCB24360 analog; Epacadostat analog
SMILES CodeO/N=C(C1=NON=C1N)/NC2=CC=C(F)C(Cl)=C2
实验参考方法
In Vitro

In vitro activity: In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 NM. In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells.


Kinase Assay: Human IDO with an N-terminal His tag was expressed in E.coli and purified to homogeneity. IDO catalyzed the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays were performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 μM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates were recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.


Cell Assay: In Hela cells, INCB024360 analogue selectively inhibited the activity of human IDO1 with an IC50 value of 19 nM. In murine B16 cells, INCB024360 analogue inhibited IDO with an IC50 value of 46 NM.

In VivoIn mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice.
Animal modelMice bearing GM-CSF-secreting B16 tumors
Formulation & DosageDissolved in 5% DMA, 47.5% propylene glycol; 75 mg/kg; s.c. administration
References

J Med Chem. 2009 Dec 10;52(23):7364-7; Blood. 2010 Apr 29;115(17):3520-30.