ETP 45658

Name: ETP 45658
Brand: Tocris Bioscience
SKU: 4702

Tocris Bioscience a Bio-Techne Brand

Catalog # 4702

Citations (2)

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Key Product Details

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)
Molecular Weight:	311.34

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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.

Solubility for ETP 45658

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	31.13	100

Preparing Stock Solutions for ETP 45658

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

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References for ETP 45658

References are publications that support the biological activity of the product.

Hill 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. 2014 PMID: 25488803
Link Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J.Biol.Chem. 2009 PMID: 19690175

Citations for ETP 45658 (2)

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Citations are publications that use Bio-Techne products. Selected citations for ETP 45658 include:

Small et al. (2022) Phenotypic screening for small molecules that protect �-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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