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.
|Source||Br J Cancer (2014). Figure 1. PKI-587|
|Cell Lines||HNSCC cell lines|
|Results||All the human squamous cell lines were highly sensitive to PKI-587, with an IC50 value ⩽100 nm|
|Solubility (25°C)||DMSO 2 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Venkatesan AM, et al. J Med Chem. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.
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