Medchemexpress LLC ETP-45658 | 1198357-79-7 | 99.0% | 311.34 | 1 ML

Supplier:  Medchemexpress LLC HY11010910MG

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. It 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.

• IC50 & Target:
  • PI3Kα: 22.0 nM (IC50)
  • PI3Kδ: 39.8 nM (IC50)
  • PI3Kβ: 129.0 nM (IC50)
  • PI3Kγ: 717.3 nM (IC50)
  • DNA-PK: 70.6 nM (IC50)
  • mTOR: 152.0 nM (IC50)
• In Vitro:
  • Decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells.
  • Inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells.
  • Induces a clear G1 arrest of PC3 cells.
  • Inhibits the mutant PI3Kα proteins, H1047R and E545K.
  • Induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells.
  • Decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells.

Catalog No. 50-003-43454