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.
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Source | PLoS One (2017). Figure 1. WYE-687 |
| Method | MTT viability assay | |
| Cell Lines | human RCC cells | |
| Concentrations | 10-1000 nM | |
| Incubation Time | 72 h | |
| Results | MTT viability assay results demonstrated that WYE-687 dose-dependently reduced786-O cell survival, and the MTT OD of 786-O cells was significantly decreasedafter10-1000 nM of WYE-687 treatment |
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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