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  3. PI3K
  4. Alpelisib hydrochloride

Alpelisib hydrochloride  (Synonyms: BYL-719 hydrochloride)

目录号: HY-15244A
产品使用指南 技术支持

Alpelisib hydrochloride (BYL-719 hydrochloride) 是有效，具有口服活性的，选择性的 PI3Kα 抑制剂，抑制 p110α/p110γ/p110δ/p110β 的 IC50 分别为 5 nM，250 nM，290 nM，1200 nM。Alpelisib hydrochloride (BYL-719 hydrochloride) 具有抗肿瘤活性。

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Alpelisib hydrochloride Chemical Structure

Alpelisib hydrochloride Chemical Structure

CAS No. : 1584128-91-5

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Alpelisib hydrochloride 的其他形式现货产品:

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Alpelisib hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 97 篇科研文献

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Cell Viability Assay
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    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17.

    Alpelisib (50 mg/kg; p.o.). Western blot and quantification of P-AKTSer473 and P-S6RP of the skin of PIK3CAWT and PIK3CATie2-CreER mice treated with either vehicle, rapamycin, miransertib or alpelisib (n = 3–4 per group).

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17.

    Alpelisib (50 mg/kg; p.o.). Representative immunofluorescence staining of KI67 in the skin of PIK3CAWT and PIK3CATie2-CreER mice treated with either vehicle, rapamycin, miransertib or alpelisib. Scale bar: 10 μm.

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Cancer Cell. 2023 Jun 12;41(6):1103-1117.e12.  [Abstract]

    Quantification of image-based cell death of organoid lines after 72 h treatment with alpelisib, idelalisib, umbralisib in indicated concentrations (0 as in DMSO vehicle control, 10, 50, and 100 μM) and bortezomib (10 μM, positive control). Cell death is estimated as the percentage of PI-positive cells out of total number of Hoechst 33342-positive nuclei, followed by normalization to the DMSO vehicle control (negative control) and positive control (bortezomib) values.

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Cancer Discov. 2023 Aug 25;CD-23-0396.  [Abstract]

    Alpelisib (50 mg/kg q.d.; administered for 3 days in the PK/PD group and 28 days in the efficacy group) reduces pAKT/AKT in the skeletal muscle of mice with CAL-33 (H1047R PI3Kα-mutant) xenograft models.

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Cancer Discov. 2023 Aug 25;CD-23-0396.  [Abstract]

    Correlation plot of alpelisib and STX-478 comparing pAKT IC50 at 1 hour and viability [CellTiter-Glo (CTGlo)] GI50 at 72 hours across the indicated panel of cell lines.

    Alpelisib hydrochloride purchased from MCE. Usage Cited in: Sci Transl Med. 2021 Oct 6;13(614):eabg0809.  [Abstract]

    Alpelisib (50 mg/kg/day; p.o.; approximately 3 months) inhibits the PI3K/AKT/mTOR pathway in lymphatic tissues of PIK3CAVEGFR3-CreER mice, reducing phosphorylation levels of AKT and S6RP.

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

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

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

    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: Oncogene. 2016 Jul 7;35(27):3607-12.  [Abstract]

    (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).

    查看 PI3K 亚型特异性产品:

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    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    体外研究
    (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Alpelisib hydrochloride 相关抗体:

    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.
    体内研究
    (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    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
    分子量

    477.93

    同用名

    BYL-719 hydrochloride

    Formula

    C19H23ClF3N5O2S
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Alpelisib hydrochloride 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Alpelisib1584128-91-5BYL-719BYL719BYL 719PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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