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  3. Alpelisib hydrochloride

Alpelisib hydrochloride (Synonyms: BYL-719 hydrochloride)

Cat. No.: HY-15244A
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Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively.

For research use only. We do not sell to patients.

Alpelisib hydrochloride Chemical Structure

Alpelisib hydrochloride Chemical Structure

CAS No. : 1584128-91-5

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Top Publications Citing Use of Products

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12.

    (A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Nature. 2018 Jun;558(7711):540-546.

    Western blot of P-AKT (Ser473), P-AKT (Thr308) and P-S6RP in liver, heart and muscles, respectively, from PIK3CAWT and PIK3CACAGG-CreER mice treated with or without BYL719 directly after Cre induction (preventive) or seven days later (therapeutic).

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2019 Jan;440-441:54-63.

    The siNC- or siBTF3-transfected breast cancer cells are treated with BYL-719 and are then subjected to an immunoblotting analysis.
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    Description

    Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively[1].

    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.
    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.
    Molecular Weight

    477.93

    Formula

    C₁₉H₂₃ClF₃N₅O₂S

    CAS No.

    1584128-91-5

    SMILES

    CC(N=C(S1)NC(N2CCC[[email protected]]2C(N)=O)=O)=C1C3=CC(C(C)(C(F)(F)F)C)=NC=C3.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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