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  3. Alpelisib

Alpelisib (Synonyms: BYL-719)

Cat. No.: HY-15244 Purity: 99.90%
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Alpelisib (BYL-719) 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 Chemical Structure

Alpelisib Chemical Structure

CAS No. : 1217486-61-7

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Alpelisib:

Top Publications Citing Use of Products

    Alpelisib 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 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 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.
    • Biological Activity

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    • Customer Review

    Description

    Alpelisib (BYL-719) 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].

    IC50 & Target[1][2]

    p110α

    5 nM (IC50)

    p110γ

    250 nM (IC50)

    p110δ

    290 nM (IC50)

    p110β

    1200 nM (IC50)

    p110α-H1047R

    4 nM (IC50)

    p110α-E545K

    4 nM (IC50)

    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.
    Clinical Trial
    Molecular Weight

    441.47

    Formula

    C₁₉H₂₂F₃N₅O₂S

    CAS No.

    1217486-61-7

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (226.52 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2652 mL 11.3258 mL 22.6516 mL
    5 mM 0.4530 mL 2.2652 mL 4.5303 mL
    10 mM 0.2265 mL 1.1326 mL 2.2652 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.90%

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    Alpelisib
    Cat. No.:
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