ChemicalBook--->CAS DataBase List--->443919-96-8

443919-96-8

443919-96-8 Structure

443919-96-8 Structure
IdentificationBack Directory
[Name]

CAY10416
[CAS]

443919-96-8
[Synonyms]

CAY10416
CAY10416,CAY-10416
3-[[3-fluoro-5-(tetrahydro-4-methoxy-2H-pyran-4-yl)phenoxy]methyl]-1-[4-(methylsulfonyl)phenyl]-5-phenyl-1H-pyrazole
1H-Pyrazole, 3-[[3-fluoro-5-(tetrahydro-4-methoxy-2H-pyran-4-yl)phenoxy]methyl]-1-[4-(methylsulfonyl)phenyl]-5-phenyl-
[Molecular Formula]

C29H29FN2O5S
[MDL Number]

MFCD12912357
[MOL File]

443919-96-8.mol
[Molecular Weight]

536.61
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 5 mg/ml
[form ]

A crystalline solid
Hazard InformationBack Directory
[Description]

Dual cyclooxygenase-2 (COX-2)/5-lipoxygenase (5-LO) inhibitors are potential therapeutic agents for inflammatory diseases and for prostate cancer. CAY10416 is a dual COX-2/5-LO inhibitor with IC50 values of 50 and 3 nM, respectively. The selectivity of CAY10416 for COX is greater than 200-fold for COX-2 versus COX-1. COX-2/5-LO inhibitors such as CAY10416 are also apoptosis-inducing agents and are potentially useful in prostate cancer chemotherapy. In the PC3 human carcinoma cell line, CAY10416 exhibits a 45% inhibition of proliferation at 100 μM. In the LNCaP human carcinoma cell line, CAY10416 inhibits growth with an IC50 value of 83 μM.
[Uses]

3-[[3-fluoro-5-(tetrahydro-4-methoxy-2H-pyran-4-yl)phenoxy]methyl]-1-[4-(methylsulfonyl)phenyl]-5-phenyl-1H-pyrazole is a dual inhibitor of Cox-2 and 5-LO.
[References]

[1] SABINE BARBEY . Synthesis and Activity of a New Methoxytetrahydropyran Derivative as Dual Cyclooxygenase-2/5-Lipoxygenase Inhibitor[J]. Bioorganic & Medicinal Chemistry Letters, 2002, 12 5: Pages 779-782. DOI: 10.1016/s0960-894x(02)00013-6
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