PI-828

PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.

Product information

CAS Number: 942289-87-4

Molecular Weight: 322.36

Formula: C19H18N2O3

Chemical Name: 8-(4-aminophenyl)-2-(morpholin-4-yl)-4H-chromen-4-one

Smiles: NC1C=CC(=CC=1)C1=CC=CC2C(=O)C=C(OC=21)N1CCOCC1

InChiKey: WUKMIBOGGXMBAC-UHFFFAOYSA-N

InChi: InChI=1S/C19H18N2O3/c20-14-6-4-13(5-7-14)15-2-1-3-16-17(22)12-18(24-19(15)16)21-8-10-23-11-9-21/h1-7,12H,8-11,20H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PI-828 (0.01-100 μM) exhibits cytotoxic effect on the 4T1 breast cancer cells and 4306 ovarian cancer cells. PI-828 (0.78-3.12 µM; 48 hours) decreases caspase 3 activation; higher concentrations of PI-828 (6.25-12.5 μM) alone causes apoptosis.

References:

1. Zellefrow CD, et al. Identification of druggable targets for radiation mitigation using a small interfering RNA screening assay. Radiat Res. 2012 Sep;178(3):150-9.
2. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21.
3. Kulkarni AA, et al. Supramolecular nanoparticles that target phosphoinositide-3-kinase overcome insulin resistance and exert pronounced antitumor efficacy. Cancer Res. 2013 Dec 1;73(23):6987-97.

Products are for research use only. Not for human use.