CAY10763 |
| カタログ番号GC47061 |
IDO1とSTAT3活性化の二重阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2364458-49-9
Sample solution is provided at 25 µL, 10mM.
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CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50 = 46 nM) and STAT3 activation.1 It binds to STAT3 (Kd = 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, 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)
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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