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PIK-75 Hydrochloride is a PI3K p110α specific inhibitor with IC50s of 6,1300,76,510 nM for p110α,p110β,p110γ, p110δrespectively.PIK-75 is a competitive inhibitor with respect to a substrate, phosphatidylinositol (PI) in contrast to most other PI3K inhibitors, which bind at or near the ATP site.
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Source | Int J Oncol (2014). Figure 2. PIK-75 |
| Method | qRT-PCR | |
| Cell Lines | AsPC-1 cells | |
| Concentrations | 0.1 μM | |
| Incubation Time | 24 h | |
| Results | PIK-75 was the most potent inhibitor that reduced the ARE-Luc reporter expression upto ~50% either in the absence or presence of exogenous FLAG-NRF2 |
| Cell Experiment | |
|---|---|
| Cell lines | LN229:EGFR (PTENwt) and U87:EGFR (PTENmt) cells |
| Preparation method | Cell proliferation assay and flow cytometry. For viability, 105 cells were seeded in 12-well plates in the presence of erlotinib, PI-103, PIK-90, rapamycin, erlotinib plus PIK-90, erlotinib plus rapamycin, erlotinib plus PIK-90, and rapamycin or erlotinib plus PI-103 for 72 h. Cell viability was determined using a WST-1 assay (Roche Molecular Biochemicals). |
| Concentrations | 0, 0.1, 0.5, 1µM |
| Incubation time | 72h |
| Animal Experiment | |
|---|---|
| Animal models | Human primary GBM43 cells female BALB/c nu/nu mice bearing xenografts model |
| Formulation | DMSO:H20 |
| Dosages | 40 mg/kg |
| Administration | daily i.p. |
| Molecular Weight | 488.74 |
| Formula | C16H14BrN5O4S.HCl |
| CAS Number | 372196-77-5 |
| Solubility (25°C) | DMSO 7 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 |
|---|
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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