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。 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
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BAY 2416964
CAS number：2242464-44-2 molecular formula：C18H18ClN5O3
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| Chinese alias | - | ||
| English alias | 4-Pyridazinecarboxamide,6-(4-chlorophenyl)-2,3-dihydro-N-[(1S)-2-hydroxy-1-methylethyl]-2-(1-methyl-1H-pyrazol-4-yl)-3-oxo- | ||
| CAS number | 2242464-44-2 | molecular formula | C18H18ClN5O3 |
| molecular weight | 387.82 g/mol | Exact mass | 10mM in DMSO |
| PSA | 99.800 Ų | logp | 1.55 |
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