ETP 45658

Pricing Availability Delivery Time Qty
Cat.No. 4702 - ETP 45658 | CAS No. 1198357-79-7
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 (1)
Literature

Biological Activity

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.

Compound Libraries

ETP 45658 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 311.34. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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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View all PI 3-kinase Inhibitors

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, PI, 3-Kinase, mTOR, DNA-dependent, Protein, Kinase, PI, 3-Kinase, Tocris Bioscience

1 Citation for ETP 45658

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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