PKI-587 (PF-05212384) is a highly potent dual PI3K/mTOR kinase inhibitor.PKI-587 (PF-05212384)potently inhibited class I PI3Ks (IC (50) vs. PI3K-α = 0.4 nmol/L), PI3K-α mutants, and mTOR.PKI-587 (PF-05212384) inhibited growth of 50 diverse human tumor cell lines at IC (50) values of less than 1nm.PKI-587 (PF-05212384) also inhibit 236 human protein kinases (IC50s >10 μM.Only wild type and mutant (V600E) B-Rafs were inhibited by PKI-587 at IC50 values of 10μM.
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Source | Br J Cancer (2014). Figure 1. PKI-587 |
| Method | MTT assay | |
| Cell Lines | HNSCC cell lines | |
| Concentrations | 10–5000 nm | |
| Incubation Time | - | |
| Results | All the human squamous cell lines were highly sensitive to PKI-587, with an IC50 value ⩽100 nm |
| Molecular Weight | 615.73 |
| Formula | C32H41N9O4 |
| CAS Number | 1197160-78-3 |
| Solubility (25°C) | DMSO 2 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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