All AbMole products are for research use only, cannot be used for human consumption.
Apitolisib (GDC-0980; GNE 390; RG 7422) is a potent, highly selective, oral, dual inhibitor of class I PI3K and mTOR. Apitolisib (GDC-0980) demonstrates broad preclinical activity in breast, ovarian, lung, and prostate cancer models. Apitolisib (GDC-0980) can potently inhibit for isoforms of p110 including p110-alpha, p110-beta, p110-gamma and p110-delta. The IC50 value for inhibition of p110-alpha, p110-beta, p110-gamma and p110-delta by GDC-0980 is 5 nM,27 nM,7 nM and 14 nM. Besides the inhibition of Phosphoinositide 3-kinase, GDC-0980 also show strong inhibition to mTOR, which is a downstream target of akt but not only in PI3K signaling pathway. The Ki value for mTOR is 17 nM.
 |
Source | Biochem Biophys Res Commun (2014). Figure 3. GDC-0980 |
| Method | Western blotting | |
| Cell Lines | PANC-1 cells and Capan-1 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Western blotting results in Fig. 1B showed clearly that GDC-0980 (1 μM) dramatically inhibited phosphorylation of AKT (Ser-473 and Thr-308) and S6K1 (Thr-389) in both PANC-1 cells and Capan-1 cells. |
| Cell Experiment | |
|---|---|
| Cell lines | NSCLS cell lines, colon cancer cell lines and etc. |
| Preparation method | Cell viability assays Three hundred and eighty-four–well plates were seeded with 2,000 cells/well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO2 overnight (∼16 hours). Compounds were diluted in dimethyl sulfoxide to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments were tested in quadruplicate. After 4 days incubation, relative numbers of viable cells were estimated using CellTiter-Glo (Promega) and total luminescence was measured on a Wallac Multilabel Reader (PerkinElmer). The concentration of drug resulting in 50% inhibition of cell viability (IC50) or 50% maximal effective concentration (EC50) was determined using Prism software (GraphPad). For cell lines that failed to achieve an IC50 the highest concentration tested (20 μmol/L) is listed. |
| Concentrations | 0~5µM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | MCF7-neo/HER2 tumor-bearing mice |
| Formulation | 0.5% methylcellulose with 0.2% Tween-80 |
| Dosages | 7.5 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 498.6 |
| Formula | C23H30N8O3S |
| CAS Number | 1032754-93-0 |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
