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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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 311.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.21 mL||16.06 mL||32.12 mL|
|5 mM||0.64 mL||3.21 mL||6.42 mL|
|10 mM||0.32 mL||1.61 mL||3.21 mL|
|50 mM||0.06 mL||0.32 mL||0.64 mL|
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
If you know of a relevant reference for ETP 45658, please let us know.
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
Citations are publications that use Tocris products. Selected citations for ETP 45658 include:
Small et al (2022) Phenotypic screening for small molecules that protect beta -cells from glucolipotoxicity. ACS Chem.Biol. 17 1131 PMID: 35439415
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
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