PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit tumor growth by 73.0% in mice[1].
PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily for 30 d) dose dependently suppresses tumor growth by 62.5% (15 mg/kg), 86.0% (30 mg/kg) and 90.7% (40 mg/kg), respectively in mice[1].
PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily; 1-4 h) inhibits the phosphorylation of Akt in a dose- and time-dependent manner in vivo[1].
PI3Kα-IN-4 shows high Cmax (mouse 22167, rat 2327 nM) and good bioavailability (mouse 59.4%, rat 46.9%) following oral administration (mouse 10, rat 3 mg/kg)[1].
PI3Kα-IN-4 shows t1/2 (mouse 0.99, rat 1.22 h) and low plasma clearance (mouse 4.16, rat 5.28 mL/min/kg) following intravenous injection (mouse 1, rat 1 mg/kg)[1].
| Animal Model: | BT-474 subcutaneous xenograft mice[1] |
| Dosage: | 30 mg/kg |
| Administration: | P.o. once daily for 21 days |
| Result: | Inhibited tumor growth by 73.0% and could be tolerated. |
