BYL-719

SKU: orb1226776

Description

Alpelisib (BYL-719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.(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 (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv) .

Key Properties

• CAS Number: 1217486-61-7
• MW: 441.47
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₂F₃N₅O₂S
• SMILES: O=C(N1[C@H](C(N)=O)CCC1)NC2=NC(C)=C(C3=CC(C(C)(C)C(F)(F)F)=NC=C3)S2
• Target: PI3K
• Solubility: Ethanol: 2 mg/mL (4.53 mM); DMSO: 88 mg/mL (199.33 mM)

Bioactivity

• In Vivo:
  Animal model: A 5-week-old female Rj: NMRI-nude mice withhuman HOS-MNNG osteosarcoma cells; A 5-week-old male C57Bl/6J mice with mouse MOS-J osteosarcoma cells. 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; 22 or 29 days for C57Bl/6J mice or Rj: NMRI-nude mice. Result: Significantly reduced tumor volumes and simultaneously reduced tumor growth. Animal model: Female Sprague Dawley rats. Dosage: 1 mg/kg (Pharmacokinetic Analysis). Administration: I. V. Result: t1/2 = 2.9±0.2 hours.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Alpelisib

Quick Database Links

Gene Symbol

PI3K