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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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SNV4818 is a potential best-in-class (best-in-class) mutation-selective PI3K-α inhibitor with excellent selectivity for the H1047X mutant and moderate selectivity for the related E545/542X mutant. |
| hSMG-1 inhibitor 11j
hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. |
| RLY-2608
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| PI3Kδ-IN-13
PI3Kδ-IN-13 is a PI3Kδ inhibitor (IC50=2.6 nM). |
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