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    Alpelisib
    Alpelisib

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    This product is for research use only, not for human use. We do not sell to patients.
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    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.

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    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


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    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.


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