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Alpelisib hydrochloride  (Synonyms: BYL-719 hydrochloride)

目录号: HY-15244A
产品使用指南

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/p110βIC50 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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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 78 篇科研文献

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    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).
    • 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.

    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

    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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    Help & FAQs
    • 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.

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