Catalog No.: PC-24655Not For Human Use, Lab Use Only.
Casdatifan (AB521) is a potent, allosteric small molecule inhibitor of protumourigenic HIF-2α, potently and selectively inhibits HIF-2α-mediated transcription with IC50 of 28.9 nM in 786-O ccRCC cells (VEGF secretion inhibition).
Casdatifan (AB521) is a potent, allosteric small molecule inhibitor of protumourigenic HIF-2α, potently and selectively inhibits HIF-2α-mediated transcription with IC50 of 28.9 nM in 786-O ccRCC cells (VEGF secretion inhibition).
AB521 binds the PAS-B domain of HIF-2α, effectively inhibiting HIF-2α-ARNT complex formation and HIF-2α-mediated transcription.
AB521 selectively inhibits HIF-2α and not HIF-1α.
AB521 inhibits HIF-2α-dependent gene expression in primary human macrophages and endothelial cells.
AB521 blocks HIF-2α-mediated gene transcription in vivo and inhibits tumour growth.
