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CAS No.: 914471-09-3

INCB024360 类似物 Catalog No. CSN15728

Synonyms: INCB14943;INCB024360-analog;INCB24360-analog

INCB024360 analogue is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述IDO1 (Indoleamine 2,3-dioxygenase-1) is a heme-containing monomeric oxidoreductase, which can catalyze the degradation of the essential amino acid tryptophan to N-formyl-kynurenine, an intermediate metabolized through a series of steps to form NAD⁺. IDO1 is considered to play an important role in the induction of tumor immune tolerance, which can regulate the immunosuppressive mechanisms responsible for tumor escape from host immune surveillance. INCB024360 Analogue, optimized from Epacadostat, is a selective IDO1 inhibitor with IC50 value of 67nM and 19nM on inhibition of IDO enzymic activity in the standard enzymatic assay and a HeLa cellular assay measuring kynurenine formation spectrophotometrically. Subcutaneous injection with INCB024360 analogue at 75mg/kg, BID, achieved 50% tumor growth control in C57BL/6 mice bearing GM-CSF-secreting B16 tumors.
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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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动物研究
剂量
Mice: min = 25 mg/kg, max = 100 mg/kg (s.c.) 25 mg/kg - 100 mg/kg (p.o.)

给药途径
s.c., p.o.

动物研究
剂量	Mice: min = 25 mg/kg, max = 100 mg/kg (s.c.) 25 mg/kg - 100 mg/kg (p.o.)
给药途径	s.c., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6813 mL
- 18.4067 mL
- 36.8134 mL
- 5 mM
- 0.7363 mL
- 3.6813 mL
- 7.3627 mL
- 10 mM
- 0.3681 mL
- 1.8407 mL
- 3.6813 mL

技术信息

CAS号

914471-09-3

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H7ClFN5O2

运输

蓝冰

分子量

271.64

别名

INCB14943;INCB024360-analog;INCB24360-analog;Epacadostat-analog. IDO-IN-2

溶解度

DMSO	500.0 mg/mL (1840.7 mM)
Water	insoluble

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

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