Molecular Weight(MW): 519.6
WYE-125132 (WYE-132) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.
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SW620 and SW620:8055R cells were treated with increasing concentrations of WYE-125132 for 24 hours and cell proliferation was assayed by [3H]thymidine incorporation. Results are the mean盋oV for three biological replicates from a single experiment; identical results were obtained in n=3 experiments.
J Cell Sci 2014 127(Pt 4), 788-800. WYE-125132 (WYE-132) purchased from Selleck.
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|Description||WYE-125132 (WYE-132) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.|
|Features||A highly potent, ATP-competitive, and specific mTOR kinase inhibitor.|
WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases.  In vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). Besides, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size.  WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover, WYE-125132 is also found to induce the dephosphorylation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus. 
|In vivo||WYE-125132 (5 mg/kg p.o.) produces significant antitumor activity and causes dose-dependent tumor growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumor model. In addition, WYE-125132 also shows potent antitumor efficacy in the PTEN-null glioma U87MG, non-small cell lung cancer H1975 and A549 models. |
Kinase assays:mTOR enzyme assays via dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA), ATP matrix assays, and mTOR immune-complex kinase assays are performed as follows. The endogenous TOR of LNCap cell lysate is immunoprecipitated by anti-FRAP/TOR (N-19). Cell lysate (1.0 mg) is mixed with 4 μg antibody coupled to protein-G/A agarose in 1 mL lysis buffer. The immune-complexes are washed sequentially with lysis buffer, lysis buffer plus 500 mM KCl, and kinase buffer wash. The immune-complexes are subjected to kinase reaction for 30 minutes at 30 °C in a final volume of 50 μL containing 10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, and 0.5 μM microcystin LR, 1 mM DTT, 10 mM MnCl2, 100 μM ATP, 1 μg His6-S6K or 1 μg His6-4EBP1. Kinase reactions (immune-complex and purified enzymes) are terminated by NuPAGE LDS sample buffer and resolved in a 4-12% NuPAGE Bis-Tris gel for Western blotting with anti-P(T389)-p70S6K and anti-P(T46)-4EBP1, anti-FRAP/TOR (N-19), anti-FLAG M2, and anti-His6 (Clone His-1). In the radioactive assay, 10 μCi [γ-32P]ATP (3000 Ci/mmol) and 100 μM cold ATP are used. 32P-labeled products are resolved by SDS-PAGE and subjected to autoradiogram to Kodak X-ray films.
|In vitro||DMSO||104 mg/mL (200.15 mM)|
|In vivo||Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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