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ChemicalBook--->CAS DataBase List--->2364458-49-9

2364458-49-9

2364458-49-9 Structure

2364458-49-9 Structure
IdentificationBack Directory
[Name]

Benzenepropanamide, α-[[1,4-dihydro-4-(hydroxyimino)-1-oxo-2-naphthalenyl]amino]-N-(3,5-dimethoxyphenyl)-, (αR)-
[CAS]

2364458-49-9
[Synonyms]

CAY10763
Benzenepropanamide, α-[[1,4-dihydro-4-(hydroxyimino)-1-oxo-2-naphthalenyl]amino]-N-(3,5-dimethoxyphenyl)-, (αR)-
[Molecular Formula]

C27H25N3O5
[MOL File]

2364458-49-9.mol
[Molecular Weight]

471.51
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
[form ]

A solid
Hazard InformationBack Directory
[Biological Activity]

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.
[References]

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)
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