GDC-0326 - 10mM in DMSO , CAS No.1282514-88-8
p110δ Selective Inhibitors
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p110δ Selective Inhibitors
Information
GDC-0326 is a potent and selective inhibitor ofPI3Kαwith Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.
Targets
PI3Kα (Cell-free assay); PI3Kδ (Cell-free assay); PI3Kγ (Cell-free assay); PI3Kβ (Cell-free assay) 0.2 nM(Ki); 4 nM(Ki) ;10.2 nM(Ki); 26.6 nM(Ki)
In vitro
In addition to achieving selectivity over the other class I isoforms, the PI3Kα specific inhibitor GDC-0326 also achieves a very high level of selectivity over other kinases. GDC-0326 is not an inhibitor of cytochrome P450 enzymes tested.
In vivo
GDC-0326 has consistently low clearance and high oral bioavailability across species tested, enabling significant sustained free drug levels.
Cell Research(from reference)
Cell lines:βTC3 cells
Concentrations:1 μM
Incubation Time:2 h
| CAS | 1282514-88-8 |
|---|---|
| Concentración | 10mM in DMSO |
| Sinónimos | SCHEMBL1485471 | AKOS030621797 | A901393 | (S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide | (25)-2-(2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-y |
| Especificaciones y pureza | 10mM in DMSO |
| Condiciones de almacenamiento de almacenamiento | Store at -80°C |
| Enviado en | Dry ice packs + Cold packs |
| Product Description | Information GDC-0326 is a potent and selective inhibitor ofPI3Kαwith Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays. Targets PI3Kα (Cell-free assay); PI3Kδ (Cell-free assay); PI3Kγ (Cell-free assay); PI3Kβ (Cell-free assay) 0.2 nM(Ki); 4 nM(Ki) ;10.2 nM(Ki); 26.6 nM(Ki) In vitro In addition to achieving selectivity over the other class I isoforms, the PI3Kα specific inhibitor GDC-0326 also achieves a very high level of selectivity over other kinases. GDC-0326 is not an inhibitor of cytochrome P450 enzymes tested. In vivo GDC-0326 has consistently low clearance and high oral bioavailability across species tested, enabling significant sustained free drug levels. Cell Research(from reference) Cell lines:βTC3 cells Concentrations:1 μM Incubation Time:2 h |
| Pubchem Sid | 528764583 |
| Objetivo | PIK3CA |
| PubChem CID | 58204997 |