VU0487836 is a selective cyclooxygenase-1 ( COX-1 ) inhibitor with an IC50 of 0.36 μM against ovine-derived COX-1. VU0487836 serves as a prototype for the development of radiological imaging agents targeting COX-1 for ovarian cancer. VU0487836 is applicable to relevant research on ovarian cancer [1].
In Vitro, VU0487836 (compound 27) potently and selectively inhibits purified ovine COX-1 with an IC50 of 0.36 μM, while it shows no inhibitory activity against purified murine COX-2 (IC50 >25 μM)[1]. VU0487836 potently and selectively inhibits COX-1 in human ovarian cancer cell line OVCAR3 with an IC50 of 0.18 μM, while it shows no inhibitory activity against COX-2 in human 1483 head and neck squamous cell carcinoma cells (IC50 >5 μM)[1].
References:
[1]. Uddin MJ, et al. Design of Fluorine-Containing 3,4-Diarylfuran-2(5H)-ones as Selective COX-1 Inhibitors. ACS Med Chem Lett. 2014 Oct 12;5(11):1254-8.
In Vitro, VU0487836 (compound 27) potently and selectively inhibits purified ovine COX-1 with an IC50 of 0.36 μM, while it shows no inhibitory activity against purified murine COX-2 (IC50 >25 μM)[1]. VU0487836 potently and selectively inhibits COX-1 in human ovarian cancer cell line OVCAR3 with an IC50 of 0.18 μM, while it shows no inhibitory activity against COX-2 in human 1483 head and neck squamous cell carcinoma cells (IC50 >5 μM)[1].
References:
[1]. Uddin MJ, et al. Design of Fluorine-Containing 3,4-Diarylfuran-2(5H)-ones as Selective COX-1 Inhibitors. ACS Med Chem Lett. 2014 Oct 12;5(11):1254-8.