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Alpelisib

(別名: BYL-719)
130 Cited Publications
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Based on 130 publication(s) in Google Scholar

Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome.

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  • 純度: 99.88%
  • CAS 番号: 1217486-61-7
  • 分子式: C19H22F3N5O2S
  • 分子量:441.47
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Alpelisib Chemical Structure
    Alpelisib 構造式
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
  • Experimental Validation Results for Alpelisib
CAS 番号: 1217486-61-7
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  • Alpelisib Chemical Structure
    Alpelisib Chemical Structure
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    Alpelisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Combined Palbociclib- and Fulvestrant-resistant cells, M-S and T-S, and the corresponding resistant cells, MPF-R and TPF-R, were treated with different inhibitors of the PI3K/AKT/mTOR pathway including Alpelisib (HY-15244; Alp; 1 μM in M-S/MPF-R and 250 to 500 nM in T-S/TPF-R), Capivasertib (Cap; 250 to 500 nM in M-S/MPF-R and 100 nM in T-S/TPF-R), Sapanisertib (Sap; 10 nM in M-S/MPF-R and 5 nM in T-S/TPF-R), and Gedatolisib (HY-10681; Ged; 10 nM) in combination with Palbociclib (HY-50767; Palbo; 200 nM) and Fulvestrant (HY-13636; Fulv; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Combined Palbociclib- and Fulvestrant-resistant cells (wild type ER+ breast cancer cells), ZPF-R, and the corresponding sensitive cells, Z-S, were treated with different inhibitors of PI3K/AKT/mTOR including Alpelisib (HY-15244; 6 μM), Capivasertib (50 nM), Sapanisertib (5 nM), and Gedatolisib (HY-10681; 5 nM) in combination with Palbociclib (HY-50767; 150 nM) and Fulvestrant (HY-13636; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Triple combination with Gedatolisib (HY-10681), Palbociclib (HY-50767), and Fulvestrant (HY-13636) effectively inhibits growth of PIK3CA-mutant ER+ tumor xenografts resistant to combined palbociclib and fulvestrant. MPF-R cells (1 × 106) resistant to combined palbociclib and fulvestrant were injected into the mammary fat pads of NOG CIEA mice, and tumors were allowed to establish for 2 weeks to a size of ≈30 mm3. Mice were then treated with the combination of Fulvestrant (100 mg/kg, sc weekly), Palbociclib (25 mg/kg, oral gavage daily), and Capivasertib (100 mg/kg, oral gavage daily; n = 6) or Alpelisib (HY-15244; 25 mg/kg, oral gavage daily; n = 5). Tumor size was measured weekly. Average tumor growth curves measured weekly and Tumor volumes measured after excision.

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Gedatolisib efficiently reduced the viability of ER+ PIK3CA- or AKT1-mutant breast cancer PDOs resistant to Abemaciclib. Dose-effect curves of CDK4/6i Abemaciclib, dual PI3K/mTORi Gedatolisib (HY-10681), PI3Ki Alpelisib (HY-15244), and dual mTORC1/2i Sapanisertib at day 7 of treatment in three breast cancer PDOs, PDO-P40, PDO-P46, and PDO-P48 (n = 3 biological replicates per group), developed from ER+ breast tumors and selected because of their differing IC50 toward Abemaciclib.

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Effect of 1 μM Abemaciclib, Gedatolisib (HY-10681), Alpelisib (HY-15244), or Sapanisertib on viability of PDO-P40, PDO-P46, or PDO-P48 during 7 days of treatment. Data are presented as means ± SEM. Significant differences are calculated by one-way ANOVA test (*P < 0.05, **P < 0.01, and ***P < 0.001).

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17;9(1):146. [Abstract]

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

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 17;9(1):146. [Abstract]

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

  • 1/16

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

    Customer Validation
     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.

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Nov 1;13(11):2432-2447. [Abstract]

    Customer Validation
     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.

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2023 Nov 1;13(11):2432-2447. [Abstract]

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

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

  • 1/16

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

    Customer Validation
     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).

  • 1/16

    Alpelisib purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12. [Abstract]

    Customer Validation
     (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