ETP-45658 is a potent PI3K inhibitor, with IC₅₀s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC₅₀=70.6 nM) and mTOR (IC₅₀=152.0 nM). ETP-45658 can be used for the research of cancer^[1][2].

ETP-45658 (10 μM; 4 h) decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells^[1].
ETP-45658 inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells, with EC₅₀s of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, respectively^[1].
ETP-45658 (10 μM; 24 h) induces a clear G1 arrest of PC3 cells^[1].
ETP-45658 inhibits the mutant PI3Kα proteins, H1047R and E545K, with IC₅₀s of 16.8 nM and 13.1 nM, respectively^[1].
ETP-45658 (5 nM-11.1 μM; 1 h) induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells^[1].
ETP-45658 (10 μM; 1 h) decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

ETP-45658 (22.7 mg/kg) decreases the level of phosphorylated Akt on serine 473 in the mammary ducts of transgenic mice^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

311.34

C₁₆H₁₇N₅O₂

1198357-79-7

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 250 mg/mL (802.98 mM; Need ultrasonic)

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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: ≥ 2.08 mg/mL (6.68 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.68 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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-CD in saline)

  Solubility: ≥ 2.08 mg/mL (6.68 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.68 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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: ≥ 2.08 mg/mL (6.68 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.68 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Link W, et, al. Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J Biol Chem. 2009 Oct 9;284(41):28392-28400.

  [2]. Hill R, et, al. A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes. Breast Cancer Res. 2014 Dec 9;16(6):482.