ETP 45658
Chemical Name: 3-[1-Methyl-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-6-ylphenol
Purity: ≥98%
Biological Activity
ETP 45658 is a PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively). Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively). Inhibits proliferation of multiple cancer cell lines in vitro and reduces Akt phosphorylation levels in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
Background References
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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.
Hill et al.
Breast Cancer Res., 2014;16:482 -
Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases.
Link et al.
J.Biol.Chem., 2009;284:28392
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Citations for ETP 45658
The citations listed below are publications that use Tocris products. Selected citations for ETP 45658 include:
2 Citations: Showing 1 - 2
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Phenotypic screening for small molecules that protect �-cells from glucolipotoxicity.
Authors: Small Et al.
ACS Chem.Biol. 2022;17:1131
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Coadministration of dox. and etop. loaded in camel milk phospholipids liposomes showed increased antitumor activity in a murine model.
Authors: Maswadeh Et al.
PLoS One 2015;10:2847
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