A dual inhibitor of IDO1 and STAT3 activation
货号:ajcx22036
CAS:2364458-49-9
分子式:C27H25N3O5
分子量：471.5
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC₅₀= 46 nM) and STAT3 activation.¹It 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 B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively.

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 3J. Med. Chem.63(4)1544-1563(2020)