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Description: Potent PI 3-kinase inhibitor; also inhibits DNA-PK and mTOR
Chemical Name: 3-[1-Methyl-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-6-ylphenol
Purity: ≥98% (HPLC)
Biological Activity for ETP 45658
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 for ETP 45658
| M. Wt | 311.34 |
| Formula | C16H17N5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1198357-79-7 |
| PubChem ID | 25229608 |
| InChI Key | BJVRNXSHJLDZJR-UHFFFAOYSA-N |
| Smiles | CN2C1=NC(C3=CC(O)=CC=C3)=NC(N4CCOCC4)=C1C=N2 |
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.
Product Datasheets for ETP 45658
References for ETP 45658
References are publications that support the biological activity of the product.
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
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
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Keywords: ETP 45658, ETP 45658 supplier, ETP45658, PI3-K, kinases, inhibitors, inhibits, dna-pk, mtor, PI3Ka, PI3Kalpha, PI3Kd, PI3Kdelta, PI3Kb, PI3Kbeta, PI3Kg, PI3Kgamma, PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ, PI, 3-Kinase, mTOR, DNA-dependent, Protein, Kinase, 4702, Tocris Bioscience
2 Citations for ETP 45658
Citations are publications that use Tocris products. Selected citations for ETP 45658 include:
Maswadeh et al (2015) Coadministration of dox. and etop. loaded in camel milk phospholipids liposomes showed increased antitumor activity in a murine model. PLoS One 10 2847 PMID: 25926730
Small et al (2022) Phenotypic screening for small molecules that protect beta -cells from glucolipotoxicity. ACS Chem.Biol. 17 1131 PMID: 35439415
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