WYE-687 is an ATP-competitivemTORinhibitor with anIC₅₀of 7 nM. WYE-687 concurrently inhibits activation ofmTORC1andmTORC2. WYE-687 also inhibitsPI3KαandPI3KγwithIC₅₀s of 81 nM and 3.11 μM, respectively.

In the DELFIA measuring His6-S6K1 T389 phosphorylation, WYE-687 inhibits recombinant mTOR enzyme with an IC₅₀of 7 nM^[1]. 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^[2].

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^[2].

528.61

Solid

C₂₈H₃₂N₈O₃

1062161-90-3

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL(47.29 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.73 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.73 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.73 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。