Home / Pharmacology / Enzymes / Kinases / PI 3-kinase / PI 3-kinase Inhibitors / ETP 45658

ETP 45658

Cat. No. 4702 2 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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)
Datasheet
Citations (2)
Reviews
Literature (4)
Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data for ETP 45658

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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.

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.

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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:

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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Literature in this Area

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