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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, 10^5 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. |
| 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 |
|---|
| 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. |
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