6-(1H-Imidazol-1-yl)-N-[2-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-3-pyridazinecarboxamide, N-(2-(1,1,1,3,3,3-Hexafluoro-2-hydroxypropan-2-yl)phenyl)-6-(1H-imidazol-1-yl)pyridazine-3-carboxamide, SR 301, SR301
Orally bioavailable analog of the selective STING agonist SR-717 with good antitumor efficacy in a murine B16.F10 melanoma tumor model in vivo.
SR-301 is an orally bioavailable analog of the selective STING agonist SR-717. SR-301 shows higher potency than SR-717 by THP1-based ISRE reporter assay (EC50 = 0.6 vs. 2.1 μM, respectively) and shows good antitumor efficacy when administered orally in a murine B16.F10 melanoma tumor model in vivo (15 mg/kg/day p.o.).
Science (New York, N.Y.), 369(6506), 993-999 (2020-08-21)
Stimulator of interferon genes (STING) links innate immunity to biological processes ranging from antitumor immunity to microbiome homeostasis. Mechanistic understanding of the anticancer potential for STING receptor activation is currently limited by metabolic instability of the natural cyclic dinucleotide (CDN)
