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CAS No. : 2050524-24-6
MCE 国际站:FD223
产品活性:FD223 是一种有效且选择性的磷酸肌醇3-激酶δ (PI3Kδ) 抑制剂。FD223 显示出高效价 (IC50=1 nM) 和对其他异构体的良好选择性 (α、β 和 γ 的IC50 值分别为 51 nM、29 nM 和 37nM)。FD223通过抑制 p-AKT Ser473 有效抑制急性髓系白血病 (AML) 细胞系的增殖,从而导致细胞周期 G1 期阻滞。FD223 在 AML 等白血病的研究中具有潜力。
研究领域:PI3K/Akt/mTOR | Apoptosis
作用靶点:PI3K | Apoptosis
In Vitro: FD223 exhibits notable anti-proliferative activities in the p110δ-positive AML cell lines HL-60, MOLM-16, EOL-1 and KG-1, with the IC50 of 2.25 μM, 0.87 μM, 2.82 μM, and 5.82 μM, respectively. FD223 shows weak anti-proliferative activity against p110δ unexpressed MM.1R cell line, with the IC50 value of 23.13 μM.
FD223 (MOLM-16 cells; 0.1-5 μM; 16 hours) dose-dependently reduces phosphorylation of Akt (Ser473), which is consistent with the positive control Idelalisib, illustrating that the activity of PI3K/Akt pathway in MOLM-16 cell is blocked.
FD223 (MOLM-16 cells; 24 hours; 1-5 μM) arrests the cell cycle at the G1 phase similar to that of positive control Idelalisib.
FD223 (1-5 μM; 48 hours) dose-dependently induces cellular apoptosis.
In Vivo: FD223 (20 and 40 mg/kg; p.o, per day for 14 consecutive days) displays potent antitumor efficacy in MOLM-16 xenograft model with the tumor volume reduction of 49% at a dose of 40 mg/kg/day (po), and shows no significant toxicity in the preliminary safety assessment.
FD223 (i.v.; dose of 2 mg/kg; p.o.; 10 mg/kg rats) shows a moderate plasma clearance rate after intravenous administration with C =0.191 L•h-1•kg-1. In the po route, it shows a half-life (t1/2) of 3.74 h and a Cmax of 1104 ng/mL, good oral plasma exposures (AUC0-∞>9000 h•ng/mL) and acceptable oral bioavailability (17.6%).
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