BAY-218 (AHR antagonist 1)
(Synonyms: AHR antagonist 1) 目录号 : GC35271
BAY-218 (AHR antagonist 1)是一种新型的、选择性的、强效的AhR小分子抑制剂。BAY-218能够抑制AhR核转位、二噁英反应元件（DRE）-荧光素酶报告基因表达，以及由外源性和内源性AhR配体诱导的AhR调节靶基因表达。
Cas No.:2162982-11-6
Sample solution is provided at 25 µL, 10mM.
BAY-218 (AHR antagonist 1) is a novel, selective, and potent AhR small molecule inhibitor. BAY-218 inhibits AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression, and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands[1].
In vitro, BAY-218 (0.1, 0.3 and 1μM; 18h) is able to reverse the inhibitory effect of kynurenic acid (KA) on the production of tumor necrosis factor alpha (TNFα) by lipopolysaccharide (LPS)-stimulated human primary monocytes[2].
In vivo, BAY-218 (30mg/kg; twice daily; p.o.) enhanced the therapeutic effect of anti-PD-L1 antibody in the CT26 mouse tumor model[2].
References:
[1] Gutcher I, Kober C, Roese L, et al. Abstract 1288: Blocking tumor-associated immune suppression with BAY-218, a novel, selective aryl hydrocarbon receptor (AhR) inhibitor[J].Experimental and Molecular Therapeutics, 2019.
[2] Schmees N, Gutcher I, Irlbacher H, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides: US201716303539[P]. US11040035B2[2025-10-07].
BAY-218 (AHR antagonist 1)是一种新型的、选择性的、强效的AhR小分子抑制剂。BAY-218能够抑制AhR核转位、二噁英反应元件（DRE）-荧光素酶报告基因表达，以及由外源性和内源性AhR配体诱导的AhR调节靶基因表达[1]。
在体外实验中，BAY-218（0.1, 0.3和1μM; 18小时）能够逆转犬尿氨酸（KA）对脂多糖（LPS）刺激的人原代单核细胞产生肿瘤坏死因子α（TNFα）的抑制作用[2]。
在体内实验中，BAY-218（30mg/kg; 每日两次; 口服）在CT26小鼠肿瘤模型中增强了抗PD-L1抗体的治疗效果[2]。
| Cell experiment [1]: | |
Cell lines | Human monocytes |
Preparation Method | Human monocytes were purified by negative selection using magnetic beads from donor PBMCs and seeded at a concentration of 2×10⁵ cells/well in complete growth medium (RPMI 1640, 10% fetal calf serum). Monocytes were incubated with 10ng/mL LPS and 200mM KA, and BAY-218 was added at concentrations of 1μM, 0.3μM, and 0.1μM, followed by culturing for 18h. LPS alone served as the positive control. TNFα production in the supernatant was measured using the Meso Scale Discovery immunoassay, and the ability of BAY-218 to rescue TNFα production was calculated based on LPS stimulation and KA-induced inhibition. |
Reaction Conditions | 0.1, 0.3 and 1μM; 18h |
Applications | BAY-218 is able to reverse the inhibitory effect of kynurenic acid (KA) on the production of tumor necrosis factor alpha (TNFα) by lipopolysaccharide (LPS)-stimulated human primary monocytes. |
| Animal experiment [1]: | |
Animal models | Female Balb/c mice |
Preparation Method | Female Balb/c mice at the age of 8 weeks were assigned to the study. CT26 cells were cultivated in RPMI 1640 containing 10% fetal calf serum and were passaged at least 3 times before inoculation. Female Balb/c mice were inoculated subcutaneously in the flank with 500,000 CT26 tumor cells (50% medium/50% matrigel). After 4 days, the animals were randomized, and treatment began on day 5. The BAY-218 at 30mg/kg was dissolved in ethanol/solutol/water (10/40/50) and administered orally twice daily, in combination with 10mg/kg of the anti-PD-L1 antibody administered intraperitoneally every 3 days. Tumor size was measured using calipers to determine length (a) and width (b). |
Dosage form | 30mg/kg; twice daily; p.o. |
Applications | BAY-218 enhanced the therapeutic effect of anti-PD-L1 antibody in the CT26 mouse tumor model. |
References: | |
| Cas No. | 2162982-11-6 | SDF | |
| 别名 | AHR antagonist 1 | ||
| Canonical SMILES | O=C(C1=CC(C2=CC=C(Cl)C=C2)=NN(C3=CC=CC(F)=C3)C1=O)N[C@@H](C)CO | ||
| 分子式 | C20H17ClFN3O3 | 分子量 | 401.82 |
| 溶解度 | DMSO: ≥ 250 mg/mL (622.17 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4887 mL | 12.4434 mL | 24.8868 mL |
| 5 mM | 497.7 μL | 2.4887 mL | 4.9774 mL |
| 10 mM | 248.9 μL | 1.2443 mL | 2.4887 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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