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WYE-687

Cat. No. M1756
WYE-687 Structure
Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 560 In stock
100mg USD 900 In stock
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Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 528.6
Formula C28H32N8O3
CAS Number 1062161-90-3
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.
Wahdan-Alaswad RS et al. Mol Cancer Res. 2012 Jun;10(6):821-33. PMID: 22452883.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WYE-687 supplier, mTOR, inhibitors

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