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ETP-45658

CAS No. : 1198357-79-7

MCE 国际站：ETP-45658

产品活性：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 nM)。ETP-45658 可用于癌症研究。

研究领域：PI3K/Akt/mTOR  |  Cell Cycle/DNA Damage

作用靶点：PI3K  |  DNA-PK  |  mTOR

In Vitro: 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.

In Vivo: ETP-45658 (22.7 mg/kg) decreases the level of phosphorylated Akt on serine 473 in the mammary ducts of transgenic mice.

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