Epacadostat (INCB024360)

製品コードS7910 バッチS791012

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₁H₁₃BrFN₇O₄S
	分子量	438.23	CAS No.	1204669-58-8
Solubility (25°C)*	体外	DMSO	100 mg/mL (228.19 mM)
		Ethanol	22 mg/mL warmed with 50ºC water bath (50.2 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
in vitro	In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. ^[1]
in vivo	INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. ^[1] In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. ^[2]

製品説明

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).

in vitro

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. ^[1]

in vivo

INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. ^[1]

In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	IDO enzyme assays
キナーゼアッセイ	Human IDO with an N-terminal His tag is expressed in E.coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays are 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 are recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.
細胞アッセイ	細胞株	Jurkat cells
	濃度	50 μM
	反応時間	72 h
	実験の流れ	Jurkat cells were incubated with serially diluted epacadostat for 72 h. Their viability was measured and analyzed as percentage of the non-treated control.
動物実験	動物モデル	Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
	投薬量	~100 mg/kg, twice a day
	投与方法	p.o.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , FEBS J, 2016, doi: 10.1111/febs.13966.]

: Data from [Data independently produced by , , Cancer Immunol Immunother, 2018, 67(8):1305-1315]

: Data from [Data independently produced by , , Mol Immunol, 2018, 103:144-155]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Epacadostat stabilizes the apo-form of IDO1 and signals a pro-tumorigenic pathway in human ovarian cancer cells [ Front Immunol, 2024, 15:1346686]	PubMed: 38333210
Selective inhibition of indoleamine and tryptophan 2,3-dioxygenases: Comparative study on kynurenine pathway in cell lines via LC-MS/MS-based targeted metabolomics [ J Pharm Biomed Anal, 2024, 237:115750]	PubMed: 37804639
Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833]	PubMed: 38451784
An adverse tumor-protective effect of IDO1 inhibition [ Cell Rep Med, 2023, 4(2):100941]	PubMed: 36812891
A tryptophan metabolite prevents depletion of circulating endothelial progenitor cells in systemic low-grade inflammation [ Front Immunol, 2023, 14:964660]	PubMed: 37081894
The catalytic inhibitor epacadostat can affect the non-enzymatic function of IDO1 [ Front Immunol, 2023, 14:1134551]	PubMed: 37122718
Targeting the STAT5A/IDO1 axis overcomes radioresistance and reverses the immunosuppressive tumor microenvironment in NSCLC [ Int J Oncol, 2023, 62(1)12]	PubMed: 36453241
IDO1 Promotes the Progression of NSCLC by Regulating the Polarization of M2 Macrophages [ Int J Gen Med, 2023, 16:1713-1733]	PubMed: 37187591
Anakinra restores cellular proteostasis by coupling mitochondrial redox balance to autophagy [ J Clin Invest, 2022, 132(2)e144983]	PubMed: 34847078
IDO-1 inhibitor INCB24360 elicits distant metastasis of basal extruded cancer cells in pancreatic ductal adenocarcinoma [ Acta Pharmacol Sin, 2022, 10.1038/s41401-022-01035-w]	PubMed: 36517670

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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