[CAS NO. 942289-87-4] PI-828
PRODUCTS SPECIFICATIONS [942289-87-4]
DESCRIPTION [942289-87-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 322.36 |
| Molecular Formula | C19H18N2O3 |
| SMILES | O=C1C=C(N2CCOCC2)OC3=C(C4=CC=C(N)C=C4)C=CC=C13 |
1 Publications Citing Use of MCE
Summary
PI-828 is a dual PI3K and casein kinase 2 ( CK2 ) inhibitor with IC 50 s of 173 nM, 149 nM, and 1127 nM for p110α , CK2 , and CK2α2 in lipid kinase assay, respectively [1] .
IC50 & Target
|
p110α 173 nM (IC 50 ) |
CK2 149 nM (IC 50 ) |
CK2α2 1.127 μM (IC 50 ) |
In Vitro
PI-828 (0.01-100 μM) exhibits cytotoxic effect on the 4T1 breast cancer cells and 4306 ovarian cancer cells
[2]
.
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
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [2]
| Cell Line: | 4T1 breast cancer cells and 4306 ovarian cancer cells |
| Concentration: | 0.01, 0.1, 1, 10 and 100 μM |
| Incubation Time: | |
| Result: | Exhibited cytotoxic effect. |
Apoptosis Analysis [3]
| Cell Line: | Human embryonic carcinoma NCCIT cells |
| Concentration: | 0.78, 1.56, 3.12, 6.25, 12.5 μM |
| Incubation Time: | 48 hours |
| Result: | Concentrations of ranging from 0.78 to 3.12 µM decreased caspase 3 activation; higher concentrations caused apoptosis. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 12.5 mg/mL ( 38.78 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1021 mL | 15.5106 mL | 31.0212 mL |
| 5 mM | 0.6204 mL | 3.1021 mL | 6.2042 mL |
| 10 mM | 0.3102 mL | 1.5511 mL | 3.1021 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (3.88 mM); Clear solution
References
- [1] Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21.
- [2] 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.
- [3] 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.