Molecular Formula | C14H8FNO3S |
Molar Mass | 289.28 |
Density | 1.466 |
pKa | 7.21±0.20(Predicted) |
Storage Condition | -20℃ |
In vitro study | A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC 50 =30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM). |
In vivo study | Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rat aortic ring precontracted with Phenylephrine (3 μM), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg,p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.457 ml | 17.284 ml | 34.569 ml |
5 mM | 0.691 ml | 3.457 ml | 6.914 ml |
10 mM | 0.346 ml | 1.728 ml | 3.457 ml |
5 mM | 0.069 ml | 0.346 ml | 0.691 ml |
biological activity | CAY10505 is an effective selective PI3Kγ inhibitor that acts on neuronal cells with an IC50 of 30 nM. |
target | PI3Kγ 30 nM (IC 50 , Neurons) |
in vitro study | A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC 50=30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is examined on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analyzed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, Tested at 10 μ m). |
in vivo studies | Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, P. o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rataortic ring precontracted with Phenylephrine (3 μ M), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, P. o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation. |