BAY-218 (Synonyms: AHR antagonist 1)
目录号: PL13924 纯度: ≥99%
CAS No. :2162982-11-6
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中文名称
BAY-218
中文别名
BAY-218
英文名称
BAY-218
英文别名
BAY-218;AHR antagonist 1;(S)-6-(4-Chlorophenyl)-2-(3-fluorophenyl)-N-(1-hydroxypropan-2-yl)-3-oxo-2,3-dihydropyridazine-4-carboxamide;BCP31105;s8842;ZB1593;ClC1=CC=C(C=C1)C=1C=C(C(N(N=1)C1=CC(=CC=C1)F)=O)C(=O)N[C@H](CO)C
Cas No.
2162982-11-6
分子式
C20H17ClFN3O3
分子量
401.82
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
BAY-218 (AHR antagonist 1) 是一种芳烃受体 (AHR) 拮抗剂。 BAY-218 在 U87 胶质母细胞瘤细胞中具有 AHR 抑制活性,IC50 为 39.9 μM。BAY-218 可用于研究癌症或免疫反应失调的病症。
生物活性
BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC 50 of 39.9 μM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses.
性状
Solid
IC50 & Target[1][2]
IC50: 39.9 nM (AHR in human cell line)
体外研究(In Vitro)
BAY-218 (example 23) (72 pM-20 μM) has AHR inhibitory activity with an IC50 of 39.9 μM in in U87 glioblastoma cells.
BAY-218 (1 nM-3 μM) has CYP1A1 inhibitory activity with an IC50 of 70.7 μM in human monocytic U937 cell line.
BAY-218 (1 μM) reverses KA-induced inhibition of TNFα production by LPS stimulated human monocytes. has not independently confirmed the accuracy of these methods. They are for reference only.RT-PCR
体内研究(In Vivo)
BAY-218 (example 23) (p.o; 30 mg/kg; bid) has good anti-tumor effect combinated with aPD-L1. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Balb/c mice (subcutaneously CT26 cells)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Norbert Schmees, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides. WO2017202816A1.
溶解度数据
In Vitro: DMSO : ≥ 250 mg/mL (622.17 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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