CAY10763

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC₅₀ = 46 nM) and STAT3 activation.¹ It binds to STAT3 (K_d = 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3^Y705) over phosphorylated STAT3^S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC₅₀s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in a B16/F10 murine melanoma model and a HepG2 mouse xenograft model when administered at doses of 100 and 10 mg/kg, respectively.

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1. Huang, R., Jing, X., Huang, X., et al. Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3. J. Med. Chem. 63(4), 1544-1563 (2020).