WYE-687

WYE-687 is a highly selective, ATP-competitive small molecule inhibitor of the mechanistic target of rapamycin (mTOR), specifically inhibiting both mTORC1 and mTORC2 complexes with an IC50 of 7 nM. WYE-687 is structurally a pyrazolopyrimidine compound. It demonstrates significant anti-proliferative and pro-apoptotic activity in cancer cell lines, causing G1 cell cycle arrest and caspase-dependent apoptosis, while showing selectivity over PI3Kα (100-fold) and PI3Kγ (500-fold), as well as 24 other protein kinases. Preclinical studies report potent anti-tumor effects in models of acute myeloid leukemia and solid tumors, and reduced expression of HIF-1α and angiogenic factors. The compound is being researched primarily as an anti-cancer agent and has not reached clinical phase trials. It is supplied for research purposes by several companies under license from Pfizer or Wyeth Research[1][3][5][7][9].

Other names

WYE-687 dihydrochlorideWYE687 dihydrochlorideWYE 687 dihydrochloride