Alpelisib hydrochloride

SKU: orb1707687

Description

Alpelisib hydrochloride

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1584128-91-5
• MW: 477.93
• Purity: 97.64% (May vary between batches)
• Formula: C₁₉H₂₃ClF₃N₅O₂S
• SMILES: CC1=C(C=2C=C(C(C(F)(F)F)(C)C)N=CC2)SC(NC(=O)N3[C@H](C(N)=O)CCC3)=N1.Cl
• Target: PI3K

Bioactivity

• In Vivo:
  Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv). 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.
• In Vitro:
  Alpelisib (BYL-719) potently inhibits the two most common PIK3CA somatic mutations (H1047R, E545K; IC50s~4 nM) and significantly alters the distribution of cell cycle phases. At 25 μM for 18 hours, it induces a G0/G1 phase cell cycle arrest in human and murine osteosarcoma cell lines. Additionally, Alpelisib (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. In cells transformed with PI3Kα, it potently inhibits Akt phosphorylation (IC50=74±15 nM) and shows significantly reduced inhibitory activity in PI3Kβ or PI3Kδ isoform-transformed cells (≥15-fold compared with PI3Kα).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BYL 719 Hydrochloride, BYL719 Hydrochloride, BYL-719 Hydrochloride, BYL-719 hydrochloride, Alpelisib hydrochloride, Alpelisib Hydrochloride

Compound Identifiers

PubChem CID

139035009