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WYE-687 is a novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin (mTOR). The mammalian target of rapamycin (mTOR) is centrally involved in cell growth, metabolism, and angiogenesis. WYE-687 as one of the pyrazolopyrimidine ATP-competitive mTOR inhibitors, with significant selectivity over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold). Unlike the rapalogs, these inhibitors acutely blocked substrate phosphorylation by mTORC1 and mTORC2 in vitro and in cells in response to growth factor, amino acids, and hyperactive PI3K/AKT. Unlike the inhibitors of PI3K or dual-pan PI3K/mTOR, cellular inhibition of P-S6K1 (T389) and P-AKT (S473) by the pyrazolopyrimidines occurred at significantly lower inhibitor concentrations than those of P-AKT (T308) (PI3K-PDK1 readout), showing mTOR selectivity in cellular setting.
Molecular Weight | 528.6 |
Formula | C28H32N8O3 |
CAS Number | 1062161-90-3 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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RMC-4529 has an IC50 value of 1.0 nM against p-4E-BP1-(T37/46) in mTOR kinase cellular assay. |
WYE-687 dihydrochloride
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. |
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