My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    Alpelisib (BLY-719; Piqray; NVP-BYL719)
    Alpelisib (BLY-719; Piqray; NVP-BYL719)

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0114
    CAS #: 1217486-61-7Purity ≥98%

    Description: Alpelisib (formerly also known as BLY719; trade name: Piqray) is a novel, potent, newly approved, orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with antineoplastic activity. As of May 2019, it has been approved by FDA as the first PI3K inhibitor to treat postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer (as detected by an FDA-approved test) following progression on or after an endocrine-based regimen. PI3K inhibitor BYL719 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Clinical data suggests a disable safety profile with manageable side effects for BYL719. 

    References: Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8; Nature. 2018 Jun;558(7711):540-546.Cancer Lett. 2018 Oct 10;440-441:54-63.

    Customer Validation
    Top Publications Citing Invivochem Products
    • Citation of InvivoChem Vorinostat (V0255) by Nature 2021, 597(7874):119-125
    • Citation of InvivoChem Larotrectinib (V2599) by Cell. 2020 Nov 25;183(5):1202-1218.e25
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022: 8, eabm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3
    • Citation of InvivoChem Larotrectinib (V2599) by Cell 2020, doi: 10.1016/j.cell.2020.10.016.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, doi: 10.1126/sciadv.abm9427.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem Vitrakvi by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem APR-246 by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem LOXO-101 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem Eprenetapopt by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem  ARRY-470 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem BMH-21 (V1435) by Cell Stem Cell 2020, 26(6): 845-861.e12.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, doi: 10.1126/sciadv.abm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem V33339 Lys-SMCC-DM1 by PNAS Nexus 2022, pgac063, https://academic.oup.com/pna
    • Citation of InvivoChem 5-azacytidine by Nature 2021, PMID: 34433969
    • Citation of InvivoChem Ruxolitinib/Filgotinib/BMS-911543/Decernotinib by J Allergy Clin Immunol 2020
    • Citation of InvivoChem LGK974 /WNT974 (V1353) by  Cancer Cell 2021 Apr 12;39(4):529-547.e7.
    • Citation of InvivoChem V1386 Napabucasin (BBI-608) by J Exp Clin Cancer Res 2021 Oct 13;40(1):319.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem Epacadostat/INCB024360 (V0942) by Cancer Discov 2022: 12(4):1106-1127.
    • Citation of InvivoChem S63845 (V2797) by Cell Death and Disease 2020, 11:316.
    • Citation of InvivoChem BMS-582949 (V2668) by Cells 2020, 9(6):1472.
    • Citation of InvivoChem Apiin (V4467) by J Med Chem 2020, 63(15):8338-8358.
    • Citation of InvivoChem V0001 venetoclax by WO2021231323A1
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)441.47
    FormulaC19H22F3N5O2S
    CAS No.1217486-61-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 88 mg/mL (199.33 mM)
    Water: 2 mg/mL (4.53 mM)
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL
    Synonym/Chemical NameAlpelisib; BYL719; BYL-719; BYL 719; NVP-BYL719; NVP BYL719; NVP-BYL-719; trade name: Piqray; (2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In VitroKinase Assay: Alpelisib (NVP-BYL719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50~4 nM). Alpelisib (NVP-BYL719) 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).

    Cell Assay: Multiple myeloma cells (OPM1, OPM2, RPMI8226, U266, MM1s,MM1R) and NCI-H9290. BYL719 prominently decreases the activation of the PI3K signaling proteins (pAKT, pS6R, and pGSK), this effect are also observed in slico that BYL719 decreases the expression of the PI3K signaling proteins in a dose-dependent manner. Furthermore, BYL719 dose-dependently triggers G1 arrest and induces apoptosis in MM cells. BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway.

    In VivoBYL719(>270 mg/d) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC in human. BYL719(270mg/d) shows first signs of clinical efficacy include 1 confirmed partial response in a patient with ER+ breast cancer, and significant PET responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17 evaluated patients.
    Animal model5-week-old male C57Bl/6J mice transplanted with human osteoblastic osteosarcoma
    Formulation & Dosage12.5-50mg/kg; Oral gavage
    ReferencesBr J Haematol. 2014 Apr;165(1):89-101.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Alpelisib


    PK/PD/efficacy relationship of NVP-BYL719 in PI3Kα-dependent tumor mouse models in vivo.  2014 May;13(5):1117-29.

     Alpelisib


    Determination of NVP-BYL719 safety profile compared with pan-class I PI3K inhibitors.  2014 May;13(5):1117-29.

     Alpelisib


    PTEN mutation and PIK3CA amplification/copy number modulate response to NVP-BYL719.  2014 May;13(5):1117-29.

     Alpelisib


    A, genetic alterations in PIK3CA predict NVP-BYL719 in vivo efficacy.   B, PDX models carrying a PIK3CA mutation and/or amplification were established by implanting surgical tumor tissues from treatment-naïve cancer patients into athymic mice.  2014 May;13(5):1117-29.

     

    Alpelisib

    PIK3CA mutation is the top positive predictor for NVP-BYL719 sensitivity. A, NVP-BYL719 sensitivity profile. Scatter plot showing Amax (%) by EC50 values expressed in μmol/L of NVP-BYL719 in cell viability assays assessed on 474 cancer cell lines.  2014 May;13(5):1117-29.

     

    Alpelisib

    Alpelisib

    Alpelisib


    Identification of selectivity index of small molecule inhibitors for PIK3CA mutant versus PIK3CA wild-type (WT) cell line populations across ∼1,000 different compounds.  2014 May;13(5):1117-29.


    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?