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PKI-587 (Gedatolisib; 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 |
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| RV-1729
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