CAS:914471-09-3INCB024360 Analogue

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Synonyms: IDO5L

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

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18817579266

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18817579266

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实验数据

技术信息

CAS号

914471-09-3

储存条件

分子式

C9H7ClFN5O2

运输

蓝冰

分子量

271.64

别名

IDO5L

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

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.
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.