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Alpelisib

CAS No. : 1217486-61-7

MCE 站：Alpelisib

产品活性：Alpelisib (BYL-719) 是有效，选择性的，具有口服活性的 PI3Kα 抑制剂。Alpelisib (BYL-719) 对 PIK3CA 突变癌具有靶向性。Alpelisib (BYL-719) 抑制 p110α、p110γ、p110δ、p110β 的 IC₅₀ 分别为 5 nM，250 nM，290 nM，1200 nM。具有抗肿瘤活性。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: Alpelisib (BYL-719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC₅₀s~4 nM). Alpelisib potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC₅₀=74±15 nM) ａnd shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (≥15-fold compared with PI3Kα).
Alpelisib (BYL-719, 0-50 μM; 72 hours) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 ａnd MOS-J in a dose-dependent manner.
Alpelisib (BYL-719) significantly alters the distribution of cell cycle phases. Alpelisib (BYL-719, 25 μM; 18 hours) induces a cell cycle arrest in the G0/G1 phase of human ａnd murine osteosarcoma cell lines.

In Vivo: Alpelisib (BYL-719) (12.5 mg/kg ａnd 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice; oral administration; daily) significantly reduces tumor volumes ａnd deposition of ectopic bone matrix.
Alpelisib has moderate terminal elimination half-life (t_1/2=2.9±0.2 h) for rat (1 mg/kg, iv) .

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