BAY 2416964
规格
Cas Number | 2242464-44-2 |
规格或纯度 | 10mM in DMSO |
包装 | 1ml |
产品信息
品牌 | 阿拉丁 |
浓度 | 10mM in DMSO |
简短描述 | AhR拮抗剂 |
英文简短描述 | AhR Antagonists |
过滤标签 | Compound libraries |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | BAY 2416964(化合物 192)是一种有效的芳基烃受体(AhR)口服活性拮抗剂,IC50 为 341 nM。BAY 2416964 具有治疗实体瘤的潜力。 |
描述 |
BAY 2416964 是一种有效的,口服活性的芳基烃受体 (AHR) 拮抗剂,其 IC50 为 341 nM,可用于实体瘤的研究。详细信息请参考专利文献 WO2018146010A1 中的化合物 192。 |
英文描述 |
Information BAY 2416964 BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors. Targets AhR (Cell-free assay) 341 nM In vitro BAY 2416964 (Example 192) induces AHR-regulated gene CYP1A1 expression with IC50 of 4.30 nM in a human monocytic U937 cells. In vivo In vivo assays: BAY 2416964 (Example 192) is dissolved in Ethanol/Solutol/Water (10/40/50) and given at 30 mg/kg, QD, p.o.. The efficacy is calculated based on tumor volume. BAY 2416964 (Example 192) is shown to have the potential for solid tumour treatment. Cell Research(from reference) Cell lines:human monocytic U937 cell line Concentrations:3.1 nmol/L, 11 nmol/L, 38 nmol/L, 130 nmol/L, 470 nmol/L, 1.6 pmol/L, 5.7 pmol/L and 20 pmol/L Incubation Time:20 h |