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WYE-687

CAS No. : 1062161-90-3

MCE 站：WYE-687

产品活性：WYE-687 是一种 ATP 竞争性的 mTOR 抑制剂，IC₅₀为 7 nM。WYE-687 抑制 mTORC1 和 mTORC2 活化。WYE-687 也抑制 PI3Kα 和 PI3Kγ，IC₅₀ 分别为 81 nM 和 3.11 μM。

研究领域：PI3K/Akt/mTOR

作用靶点：mTOR  |  PI3K

In Vitro: In the DELFIA measuring His6-S6K1 T389 phosphorylation, WYE-687 inhibits recombinant mTOR enzyme with an IC₅₀ of 7 nM. HL-60 AML cells are treated with applied concentrations of WYE-687 (33-1000 nM), MTT cell survival assay results demonstrate that WYE-687 potently inhibits HL-60 cell survival in a dose-dependent manner. A time dependent response by WYE-687 is also noticed. The number of dead (“trypan blue” positive) HL-60 cells is significantly increased following applied WYE-687 (100-1000 nM) treatment. At the meantime, HL-60 cell proliferation, tested by [H³] Thymidine integration assay, is also inhibited by the WYE-687. Results show that WYE-687 is also antisurvival (“cytotoxic”) to the other AML cell lines: U937, THP-1 and AML-193.

In Vivo: U937 cells are inoculated into the flanks of SCID/beige mice. When xenografted tumors reach a volume around 100 mm³, mice are orally administrated with either vehicle control (5% ethanol, 2% Tween 80, and 5% polyethylene glycol-400) or WYE-687 (5 or 25 mg/kg) daily for a total of 7 days. The WYE-687 regimen utilized in this study is based on preexperimental results and related studies. WYE-687 administration (5 or 25 mg/kg, daily) significantly inhibits U937 xenograft tumor growth in SCID mice, and the in vivo activity by WYE-687 is dose-dependent. At day 15, the 5 mg/kg WYE-687-treated tumors and 25 mg/kg WYE-687-treated tumors are 50% and 75% smaller than the vehicle control tumors, respectively. Tumor weights of WYE-687-treated mice are also significantly lower than that of vehicle group. Oral administration of WYE-687 potently inhibits U937 leukemic xenograft tumor growth in SCID mice, without causing significant toxicities.

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