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ETP-45658


CAS No. : 1198357-79-7

1198357-79-7
Price and Availability of CAS No. : 1198357-79-7
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Cat. No. : HY-110109
M.Wt: 311.34
Formula: C16H17N5O2
Purity: >98 %
Solubility: DMSO : 250 mg/mL (ultrasonic)
Introduction of 1198357-79-7 :

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

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