| Molecular Weight: | 446.5 |
| Formula: | C24H26N6O3 |
| Purity: | ≥98% |
| CAS#: | 1220699-06-8 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | (S)-1-(1-(2-hydroxypropanoyl)piperidin-4-yl)-3-methyl-8-(6-methylpyridin-3-yl)-1H-imidazo[4,5-c][1,5]naphthyridin-2(3H)-one |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor developed through structure-based drug design. It inhibited mTOR, PI3Kα, β, δ and γ isoforms and AKT phosphorylation with IC50 as 2.64 nM, 0.395 nM, 0.111 nM, 0.122 nM and 28.3 nM, respectively. PF-04979064 exhibited cellular potency with an IC50 of 9.1 nM in a BT20 cell assay. PF-04979064 exhibited excellent in vitro potency, very good solubility, high LipE, excellent kinome selectivity, robust PK/PD correlation and tumor growth inhibition (TGI) in a U87MG mouse xenograft model, and acceptable predicted human clearance after incorporating both CYP- and AO-mediated metabolism. PF-04979064 is the back-up candidate to PF-04691502 which is in Phase I/II clinical trials for treating solid tumors.
How to Use:
- In vitro: PF-04979064 was used at 1-10 µM in vitro and in cellular assays.
- In vivo: PF-04979064 was orally dosed to mice at 15-40 mg/kg once per day for two weeks.
Reference:
- 1. Hengmiao Cheng, et al. Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. (2013) ACS Med. Chem. Lett., 4 (1), pp91-97.
Products are for research use only. Not for human use.
