GlpBio

INCB-024360

目录号: GC17968纯度: >99.50%同义词: 艾卡哚司他,INCB 024360
INCB-024360，又名epacadostat，是一种口服小分子选择性IDO1抑制剂（IC50 = 71.8nM）。
INCB-024360
Cas No.: 1204669-58-8
规格价格库存数量操作
1mg¥175.00现货
1
5mg¥350.00现货
1
10mg¥560.00现货
1
25mg¥1,050.00现货
1
50mg¥1,610.00现货
1
100mg¥2,520.00现货
1
200mg¥4,060.00现货
1
500mg¥7,700.00现货
1
10mM (in 1mL DMSO)¥385.00现货
1
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产品描述 Description

INCB-024360, also known as epacadostat, is an oral small molecule selective IDO1 inhibitor (IC50 = 71.8nM) [1]. INCB-024360 can selectively inhibit IDO1 enzyme activity and block the pathway of tryptophan metabolism to kynurenine [2]. INCB-024360 is mainly used to treat advanced or metastatic solid tumors [3-4].

In SKOV-3 cells, INCB-024360 (10-3-104nM; 24h, 48h, 72h) increases IDO1 protein expression [5]. In HT-29 cells, INCB-024360 (10μM; 96h) reduced cell viability [6]. In 4T1 cells, INCB-024360 (1μM; 24h, 48h) sensitize pulmonary metastases to agents targeting hypoxia/nutrient deprivation survival mechanisms [7].

In colon carcinoma xenograft mice model, INCB-024360 (100mg/kg; ig; 2h) effectively inhibits the metabolism of tryptophan to kynurenine by achieving high drug exposure in areas with high IDO1 expression, significantly reducing the Kyn/Trp ratio, thereby restoring immune activity and enhancing anti-tumor efficacy [8]. In in wild-type and PD-1-negative mice, co-administration of the CTLA-4 blocking antibody 9D9 and/or the IDO1 inhibitor INCB-024360 (300mg/kg; ig; 27d) (to mimic the effects of PD1 blockade) synergistically induced liver injury and immune cell infiltration [9]. In TAC-induced WT mice, INCB-024360 (50mg/kg; sc; 4 weeks) inhibits IDO1 and ameliorates pathological cardiac hypertrophy and remodeling [10].

References:
[1]. Liu X, Shin N, Koblish HK, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood, The Journal of the American Society of Hematology. 2010 Apr 29; 115(17): 3520-3230.
[2]. Hao X, Chen Z, Li H, et al. Small-molecule drugs in immunotherapy. Mini Reviews in Medicinal Chemistry. 2023 Jul 1;23(13):1341-1359.
[3]. Alford B, Cox K, Soliman H. IDO1 inhibitors for cancer immunotherapy. Drugs of the Future. 2016 Sep 1; 41(9): 553-559.
[4]. Hellmann MD, Gettinger S, Chow LQ, et al. Phase 1 study of epacadostat in combination with atezolizumab for patients with previously treated advanced nonsmall cell lung cancer. International Journal of Cancer. 2020 Oct 1; 147(7): 1963-1969.
[5]. Rossini S, Ambrosino S, Volpi C, et al. Epacadostat stabilizes the apo-form of IDO1 and signals a pro-tumorigenic pathway in human ovarian cancer cells. Frontiers in Immunology. 2024 Jan 25; 15: 1346686.
[6]. Zhou Y, Tao Q, Luo C, et al. Epacadostat Overcomes Cetuximab Resistance in Colorectal Cancer by Targeting IDO‐Mediated Tryptophan Metabolism. Cancer Science. 2025 Mar 18.
[7]. Shen SC, Dey S, DuHadaway JB, et al. Neovascular pruning by IDO1 inhibitors can potentiate immunogenic cytotoxicity of ischemia-targeted agents to synergistically enhance anti-PD-1 responsiveness. Journal for Immunotherapy of Cancer. 2025 May 30; 13(5): e011398.
[8]. Poncelet L, Ait-Belkacem R, Marillier R, et al. Target exposure and pharmacodynamics study of the indoleamine 2, 3-dioxygenase-1 (IDO-1) inhibitor epacadostat in the CT26 mouse tumor model. Journal of Pharmaceutical and Biomedical Analysis. 2019 Jun 5; 170: 220-227.
[9]. Affolter T, Llewellyn HP, Bartlett DW, et al. Inhibition of immune checkpoints PD-1, CTLA-4, and IDO1 coordinately induces immune-mediated liver injury in mice. PLoS One. 2019 May 21; 14(5): e0217276.
[10]. Wang Y, Song J, Yu K, et al. Indoleamine 2, 3-dioxygenase 1 deletion-mediated kynurenine insufficiency inhibits pathological cardiac hypertrophy. Hypertension. 2023 Oct; 80(10): 2099-2111.

INCB-024360，又名epacadostat，是一种口服小分子选择性IDO1抑制剂（IC50 = 71.8nM） [1]。INCB-024360可以选择性抑制IDO1酶活性，阻断色氨酸代谢为犬尿氨酸的途径 [2]。INCB-024360主要用于治疗晚期或转移性实体瘤 [3-4]。

在SKOV-3细胞中，INCB-024360（10-3-104nM；24h、48h、72h）可增加IDO1蛋白的表达 [5]。在HT-29细胞中，INCB-024360（10μM；96h）可降低细胞活力 [6]。在4T1细胞中，INCB-024360（1μM；24h、48h）可增强肺转移瘤对靶向缺氧/营养剥夺生存机制的药物的敏感性 [7]。

在结肠癌异种移植小鼠模型中，INCB-024360（100mg/kg；ig；2h）通过在IDO1高表达区域实现高药物暴露，有效抑制色氨酸代谢为犬尿氨酸，显著降低犬尿氨酸/色氨酸比例，从而恢复免疫活性并增强抗肿瘤疗效 [8]。在野生型和PD-1阴性小鼠中，联合应用CTLA-4阻断抗体9D9和/或IDO1抑制剂INCB-024360（300mg/kg；ig；27d）（以模拟PD-1阻断的作用）可协同诱导肝损伤和免疫细胞浸润 [9]。在TAC诱导的WT小鼠中，INCB-024360（50mg/kg；sc；4周）抑制IDO1并改善病理性心脏肥大和重塑 [10]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

SKOV-3 cells

Preparation Method

The cell viability of SKOV-3 cells exposed to INCB-024360 was analyzed by MTT assay. Cells were seeded at the final concentration of 5 x 103 cells/100µL/well in a 96-well plate, and treated with INCB-024360 for 24, 48, and 72 hours. Vehicle-treated cells were used as control. At each time point, the stimulus was removed and cells were provided with 110µL/well of complete medium containing MTT at the final concentration of 0.45mg/mL. After 4 hours at 37℃, 100µL/well of the solubilization buffer (SDS 10% in HCl 0.01M) were added and cells were incubated overnight at 37℃. The day after, cell viability was determined by measuring the absorbance at 570nm, by using a UV/visible spectrophotometer.

Reaction Conditions

10-3-104nM; 24h, 48h, 72h

Applications

INCB-024360 increases IDO1 protein expression in SKOV-3 cells.

Animal experiment [2]:

Animal models

Colon carcinoma xenograft mice model

Preparation Method

Colon carcinoma CT26 cell line was subcutaneously grafted into BALB/c mice (Charles River Laboratories, France). Mice were randomized and treatment was started when tumors had an average size of 70-120mm3. Mice were treated by oral gavage with the IDO1 inhibitor, INCB-024360 at 100mg/kg, and then sacrificed 2h later.

Dosage form

100mg/kg; ig; 2h

Applications

INCB-024360 effectively inhibits the metabolism of tryptophan to kynurenine by achieving high drug exposure in areas with high IDO1 expression, significantly reducing the Kyn/Trp ratio, thereby restoring immune activity and enhancing anti-tumor efficacy.

References:
[1]. Rossini S, Ambrosino S, Volpi C, et al. Epacadostat stabilizes the apo-form of IDO1 and signals a pro-tumorigenic pathway in human ovarian cancer cells. Frontiers in Immunology. 2024 Jan 25; 15: 1346686.
[2]. Poncelet L, Ait-Belkacem R, Marillier R, et al. Target exposure and pharmacodynamics study of the indoleamine 2, 3-dioxygenase-1 (IDO-1) inhibitor epacadostat in the CT26 mouse tumor model. Journal of Pharmaceutical and Biomedical Analysis. 2019 Jun 5; 170: 220-227.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1204669-58-8
同义词
艾卡哚司他,INCB 024360
化学名
(E)-N'-(3-bromo-4-fluorophenyl)-N-hydroxy-4-((2-(sulfamoylamino)ethyl)amino)-1,2,5-oxadiazole-3-carboximidamide
SMILES
BrC1=C(F)C=CC(/N=C(NO)\C2=NON=C2NCCNS(N)(=O)=O)=C1
分子式
C11H13BrFN7O4S
分子量
438.23 g/mol
溶解性
≥ 17.1mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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