| Name | PI3Kα-IN-4 |
| Description | PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor with an IC50 of 1.8 nM, demonstrating antitumor activity [1]. |
| In vitro | PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ in kinase assays with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively, and in cell-based assays with IC50s of 12.1, 1393, 183, and >10000 nM, respectively [1]. |
| In vivo | PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 days) achieves 73.0% tumor growth inhibition in mice. It dose-dependently suppresses tumor growth by 62.5% (15 mg/kg), 86.0% (30 mg/kg), and 90.7% (40 mg/kg) when administered orally once daily for 30 days. Time- and dose-dependent inhibition of Akt phosphorylation is observed in vivo (15-40 mg/kg; p.o. once daily; 1-4 h). The compound shows high Cmax (mouse 22167, rat 2327 nM) and good bioavailability (mouse 59.4%, rat 46.9%) after oral administration (mouse 10, rat 3 mg/kg). Following intravenous injection (mouse 1, rat 1 mg/kg), it has a t1/2 of 0.99 hours in mice and 1.22 hours in rats, with low plasma clearance (mouse 4.16, rat 5.28 mL/min/kg). |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (178.57 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (5.89 mM), Sonication is recommended.
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| Keywords | PI-3Kα-IN-4 | PI3KαIN4 | PI3Kα IN 4 | PI3Kalpha-IN-4 | PI3Ka-IN-4 |
| Inhibitors Related | Musk ketone | Myricetin | Creatine monohydrate | Hyaluronic acid | 4-Methylbenzylidene camphor | 4-Vinylcyclohexene Dioxide | Berberine hydrogen sulphate | Isoprenaline hydrochloride | Methyl eugenol | Thymoquinone | Quercetin | Berberine sulfate |
United States
