Bioactivity | BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 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[1]. | ||||||||||||
Target | IC50: 39.9 nM (AHR in human cell line) | ||||||||||||
Invitro | BAY-218 (example 23) (72 pM-20 μM) has AHR inhibitory activity with an IC50 of 39.9 μM in in U87 glioblastoma cells[1].BAY-218 (1 nM-3 μM) has CYP1A1 inhibitory activity with an IC50 of 70.7 μM in human monocytic U937 cell line[1].BAY-218 (1 μM) reverses KA-induced inhibition of TNFα production by LPS stimulated human monocytes[1]. RT-PCR[1] Cell Line: | ||||||||||||
In Vivo | BAY-218 (example 23) (p.o; 30 mg/kg; bid) has good anti-tumor effect combinated with aPD-L1[1]. Animal Model: | ||||||||||||
Name | BAY-218 | ||||||||||||
CAS | 2162982-11-6 | ||||||||||||
Formula | C20H17ClFN3O3 | ||||||||||||
Molar Mass | 401.82 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Norbert Schmees, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides. WO2017202816A1. |