CAY10763
A dual inhibitor of IDO1 and STAT3 activation
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
-
包装价格促销价数量
-
500ug￥1337.001070.00- +
-
1mg￥2562.002050.00- +
-
5mg￥10025.008020.00- +
- 货号: ajcx22036
- CAS: 2364458-49-9
- 别名:
- 分子式: C27H25N3O5
- 分子量: 471.5
- 纯度: ＞98%
- 溶解度: DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
- 储存: 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.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)
