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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, selective, and orally active PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. Alpelisib (BYL-719) shows antineoplastic activity.

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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10 mM * 1 mL in DMSO USD 66 In-stock
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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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    Description

    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. Alpelisib (BYL-719) shows antineoplastic activity[1][2].

    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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    Cat. No.:
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