PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer[1].
PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively[1].
PI3K/mTOR Inhibitor-4 (2.5-10 µM; 24 h) inhibits the PI3K/AKT/mTOR pathway[1].
Cell Viability Assay[1]
| Cell Line: | PC12 and LO2 cells |
| Concentration: | 0.625-20 µM |
| Incubation Time: | 72 h |
| Result: | Showed low toxicity in concentrations from 0.625 µM to 20 µM. |
Western Blot Analysis[1]
| Cell Line: | Hela cells |
| Concentration: | 2.5, 5 and 10 µM |
| Incubation Time: | 24 h |
| Result: | Dose-dependently decreased the level of phosphorylation of AKT and its downstream target S6 in Hela cell line. |
PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague-Dawley rats[1].
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity[1].
| Animal Model: | SD rats (male; 200-220 g)[1] | ||||||||||||||||
| Dosage: | 1, 10 mg/kg | ||||||||||||||||
| Administration: | Intravenous, oral | ||||||||||||||||
| Result: |
|
| Animal Model: | BALB/c nude mice (female; 6-7 weeks; 18-22 g)[1] |
| Dosage: | 10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model) |
| Administration: | Oral |
| Result: | Inhibited the growth of xenograft tumors in a dose-dependent manner. |