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WYE-132

CAS No. : 1144068-46-1

MCE 站：WYE-132

产品活性：WYE-132 (WYE-125132) 是一种高度有效的 ATP 竞争性和特异性 mTOR 激酶抑制剂 (IC₅₀ 为 0.19±0.07 nM)。WYE-132 (WYE-125132) 抑制 mTORC1 和 mTORC2。

研究领域：PI3K/Akt/mTOR  |  Apoptosis

作用靶点：mTOR  |  Apoptosis

In Vitro: WYE-132 (WYE-125132) potently inhibits recombinant mTOR via an ATP-competitive mechanism. WYE-132 is a potent antiproliferative agent against a panel of cancer cell lines with IC₅₀ values generally in the nanomolar range. In the typical 3-day dose-response studies, WYE-132 exhibits a more profound antiproliferative activity than CCI-779 in MDA361 ａnd other cells, as shown by the sharper inhibition at doses up to 10 μM. Fluorescence-activated cell sorting (FACS) analysis of inhibitor-treated (1 μM, 24 hours) MDA468, PC3MM2, U87MG, A549, ａnd HCT116 cells indicates that WYE-132 elicits a more profound increase in G₁-phase ａnd a reduction in S-phase cells than CCI-779. The WYE-132-induced cell death is evident at 10 ａnd 30 nM (6.2% ａnd 13%, respectively) ａnd is dose dependent, reaching 47% at 1 μM ａnd 59% at 3 μM.

In Vivo: A single i.v. administration of 50 mg/kg WYE-132 (WYE-125132) into tumor-bearing mice leads to suppression of P-S6K(T389) ａnd P-AKT(S473) for at least 8 hours in PC3MM2, MDA361, HCT116, ａnd HT29 tumors, whereas the steady-state level of P-AKT(T308) is not significantly reduced, indicating that the antitumor efficacy of WYE-132 under such dosing regimens reflects the suppression of mTOR rather than PI3K. Oral administration of WYE-132 causes dose-dependent tumor growth delay in the PI3K/mTOR- ａnd HER2-hyperactive MDA361 tumors with significant antitumor activity at 5 mg/kg, which correlates with a suppression P-S6 ａnd P-AKT(S473) but not P-AKT(T308). An optimal dose of 50 mg/kg WYE-132 induces a substantial regression of large MDA361 tumors. WYE-132 also causes a potent ａnd substantial tumor growth delay in the PTEN-null U87MG glioma.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Antioxidants Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  MG-132  |  Rapamycin  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Angiotensin II human  |  Acetylcysteine  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Verteporfin  |  Temozolomide  |  Decitabine  |  BAY 11-7082  |  Etoposide  |  CCCP  |  DAPT  |  Rote  |  Etomoxir  |  Stattic  |  Docetaxel  |  Fulvestrant  |  Everolimus

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