Alpelisib hydrochloride (BYL-719 hydrochloride) 是有效，具有口服活性的，选择性的PI3Kα抑制剂，抑制p110α/p110γ/p110δ/p110β的IC50分别为 5 nM，250 nM，290 nM，1200 nM。Alpelisib hydrochloride (BYL-719 hydrochloride) 具有抗肿瘤活性。
| 生物活性 | Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selectivePI3Kαinhibitor withIC50s of 5 nM, 250 nM, 290 nM and 1200 nM forp110α,p110γ,p110δ, andp110β, respectively. Alpelisib hydrochloride (BYL-719 hydrochloride) shows antineoplastic activity[1][2]. |
体外研究
(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)[2].
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[3].
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[3].
Cell Proliferation Assay[3] | Cell Line: | MG63, HOS, POS-1, MOS-J | | Concentration: | 10, 20, 30, 40, 50 μM | | Incubation Time: | 72 hours | | Result: | Inhibited the cell growth of all osteosarcoma cell lines tested in a dose-dependent manner with IC50s of 6-15 μM and with IC90s of 24-42 μM. |
Cell Cycle Analysis[3] | Cell Line: | MG63, HOS, POS-1, MOS-J | | Concentration: | 25 μM | | Incubation Time: | 18 hours | | Result: | Induced a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell. |
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体内研究
(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[3].
Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv)[1].
| Animal Model: | A 5-week-old female Rj:NMRI-nude mice with human HOS-MNNG osteosarcoma cells; A 5-week-old male C57Bl/6J mice with mouse MOS-J osteosarcoma cells[3] | | Dosage: | 12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice | | Administration: | Oral administration; daily | | Result: | Significantly reduced tumor volumes and simultaneously reduced tumor growth. |
| Animal Model: | Female Sprague Dawley rats[1] | | Dosage: | 1 mg/kg (Pharmacokinetic Study) | | Administration: | I.V. | | Result: | T1/2=2.9±0.2 hours. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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