Cat. No. 4702
Chemical Name: 3-[1-Methyl-4-(4-morpholinyl)-1H-py
Biological ActivityPI 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Hill et al (2014) 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. 16 482. PMID: 25488803.
Link et al (2009) Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J.Biol.Chem. 284 28392. PMID: 19690175.
If you know of a relevant reference for ETP 45658 please let us know.
Citations are publications that use Tocris products. Selected citations for ETP 45658 include:
Maswadeh et al (2015) Coadministration of doxorubicin and etoposide loaded in camel milk phospholipids liposomes showed increased antitumor activity in a murine model. PLoS One 10 2847. PMID: 25926730.
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Keywords: ETP 45658, supplier, ETP45658, PI3-K, kinases, inhibitors, kinases, inhibits, dna-pk, mtor, PI3Ka, PI3Kalpha, PI3Kd, PI3Kdelta, PI3Kb, PI3Kbeta, PI3Kg, PI3Kgamma, PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ, Tocris Bioscience, PI 3-kinase Inhibitor products
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