ETP-45658 是一种有效的 PI3K 抑制剂，抑制 PI3Kα，PI3Kδ，PI3Kβ 和 PI3Kγ的 IC₅₀ 值分别为 22.0 nM，39.8 nM，129.0 nM 和 717.3 nM。ETP-45658 还可以抑制 DNA-PK (IC₅₀=70.6 nM) 和 mTOR (IC₅₀=152.0

ETP-45658 is a potent PI3K inhibitor, with IC 50 s 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 (IC 50 =70.6 nM) and mTOR (IC 50 =152.0 nM). ETP-45658 can be used for the research of cancer.

Solid

PI3Kα 22.0 nM (IC50) PI3Kδ 39.8 nM (IC

ETP-45658 (10 μM; 4 h) decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells.
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.
ETP-45658 (10 μM; 24 h) induces a clear G1 arrest of PC3 cells.
ETP-45658 inhibits the mutant PI3Kα proteins, H1047R and E545K, with IC50s of 16.8 nM and 13.1 nM, respectively.
ETP-45658 (5 nM-11.1 μM; 1 h) induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells.
ETP-45658 (10 μM; 1 h) decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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 De

In Vitro: DMSO : 250 mg/mL (802.98 mM; Need ultrasonic)配制储备液