BAY-2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY2416964 specifically binds to AhR, inhibits AhR activation, and prevents AhR-mediated signaling. Abrogation of AhR activation prevents the activation of immune-tolerant dendritic cells (DCs) and regulatory T cells (Tregs) in the tumor microenvironment (TME). This may restore the immune response against tumor cells.
Chemical Formula: C18H18ClN5O3
Exact Mass: 387.1098
Molecular Weight: 387.824
Elemental Analysis: C, 55.75; H, 4.68; Cl, 9.14; N, 18.06; O, 12.38
Chemical Name: (S)-6-(4-chlorophenyl)-N-(1-hydroxypropan-2-yl)-2-(1-methyl-1H-pyrazol-4-yl)-3-oxo-2,3-dihydropyridazine-4-carboxamide
InChi Code: InChI=1S/C18H18ClN5O3/c1-11(10-25)21-17(26)15-7-16(12-3-5-13(19)6-4-12)22-24(18(15)27)14-8-20-23(2)9-14/h3-9,11,25H,10H2,1-2H3,(H,21,26)/t11-/m0/s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
BAY 2416964 (Example 192) induces AHR-regulated gene CYP1A1 expression in a human monocytic U937 cells with an IC50 of 4.3 nM.
IlonaGUTCHER,etal.2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer. WO2018146010A1
Products are for research use only. Not for human use.
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