WYE-687

WYE-687 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.007 µM).1 It is selective for mTOR over PI3Kα and PI3Kγ (IC50s = 0.81 and 3.11 µM, respectively), as well as a panel of 24 additional kinases (IC50s = >50 µM for all). WYE-687 (0.2, 1, and 5 µM) decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1) in a cell-free assay. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.18 to 1.25 µM. WYE-687 inhibits survival of HL-60 and U937 leukemia cells in a concentration-dependent manner and reduces tumor growth in a U937 mouse xenograft model when administered at doses of 5 and 25 mg/kg.2WARNING This product is not for human or veterinary use.

An mTOR inhibitor

528.6

≥98%

Biochemicals/Kinase Inhibitors/mTOR/Small Molecule Inhibitors/Kinases

Formal_Name:N-[4-[4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-carbamic acid, methyl ester;Synonyms:WAY-687

O=C(OC)NC1=CC=C(C2=NC(N3CCOCC3)=C(C=NN4C5CCN(CC6=CN=CC=C6)CC5)C4=N2)C=C1

C28H32N8O3

1062161-90-3

≥ 4 years

DMSO: soluble