| Description | PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM) |
| In vitro | PI3K/mTOR Inhibitor-1 (Compound 26) as a potent dual PI3K/mTOR inhibitor.?It exhibited high inhibitory activity against PI3Kα/β/γ/δ (IC50 = 20/376/204/46 nM) and mTOR (IC50 = 189 nM), potent functional suppression of AKT phosphorylation (IC50 = 196 nM), and excellent antiproliferative effects on a panel of cancer cells.?Enzymic data and modeling simulation indicate that a cyclopropyl ring on the C4 sulfone chain and a fluorine on the C6 aminopyridyl moiety are responsible for its maintained PI3K activity and enhanced mTOR potency, respectively. |
| In vivo | PI3K/mTOR Inhibitor-1 (Compound 26) exhibited higher efficiency(antiproliferative effects) in the HT-29 colorectal carcinoma xenograft model at the daily dose of 3.75 and 7.5 mg/kg relative to BKM120 at the dose of 15 and 30 mg/kg. |
| Target activity | mTOR:186 nM, PI3Kγ:204 nM, PI3Kα:20 nM, PI3Kβ:376 nM, PI3Kδ:46 nM |
| molecular weight | 407.46 |
| Molecular formula | C18H22FN5O3S |
| CAS | 1949802-49-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Shen S, et al. Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. ACS Med Chem Lett. 2018 Jun 25;9(7):719-724. |