240427-90-1

20-HEDE (WIT 002).

ω-hydroxylation activity toward arachidonic acid is high in A549 cells, thus, A549 cells are treated with HET0016 or WIT 002 in the invasion assays, and both of them significantly decrease invasion. WIT 002 inhibits proliferation of 786-O and 769-P renal adenocarcinoma cells, but HET0016 and WIT 002 fail to inhibit proliferation of normal renal epithelial cells RPTC.

The effect of the 20-HETE antagonist, WIT 002 on the growth of 786-O clear cell renal carcinoma is assessed in ectopic mouse model of renal tumor. The growth of tumors is significantly suppressed by WIT 002 administered daily to athymic nude mice implanted subcutaneously with cells 786-O. Tumor growth is inhibited by 84%±128%. It is of note that in these experiments WIT 002 treatment start only after the tumor is seeded for 7-14 days and is relatively large 0.1 cm. Thus, WIT 002 is effective at arresting the growth of a fairly advanced tumor.