1. PI3K/Akt/mTOR
  2. PI3K

BYL-719 (Synonyms: Alpelisib)

Cat. No.: HY-15244 Purity: 99.04%
Data Sheet SDS Handling Instructions

BYL-719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM.

For research use only. We do not sell to patients.
BYL-719 Chemical Structure

BYL-719 Chemical Structure

CAS No. : 1217486-61-7

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Customer Review

    BYL-719 purchased from MCE. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12.

    (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).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BYL-719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM.

    IC50 & Target

    IC50: 5 nM (p110α), 250 (p110γ), 290 (p110δ), 1200 (p110β)[1]

    In Vitro

    BYL-719 (NVP-BYL719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50~4 nM). BYL-719 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]. BYL-719 (BYL719) decreases cell proliferation by blocking cell cycle in G0/G1 phase with no outstanding effects on apoptosis cell death in HOS and MOS-J tumor cells. BYL-719 inhibits cell migration and can thus be considered as a cytostatic drug for osteosarcoma. In murine preclinical models of osteosarcoma, BYL-719 significantly decreases tumor progression and tumor ectopic bone formation as shown by a decrease of Ki67+ cells and tumor vascularization. BYL-719 rapidly inhibits the levels of P-AKT and P-mTOR in all cell lines assessed, confirming the functional activity of BYL-719 on osteosarcoma cells. After 72 hr of treatment, BYL-719 significantly inhibits the cell growth of all osteosarcoma cell lines tested in a dose-dependent manner with an IC50 ranging from 6 to 15 µM and with the IC90 from 24 to 42 µM at 72 hr[3].

    In Vivo

    BYL-719 displays excellent oral bioavailability in rats, mice and dogs and does not show any significant inhibition of the CYP450 enzymes[1]. BYL-719 (BYL719) inhibits tumor growth in pre-clinical murine models of osteosarcoma. C57Bl/6J with MOS-J tumors (n=6 per group) are randomized as controls (vehicle) or BYL-719 (12.5 mg/kg or 50 mg/kg per day)[3].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT03207529 M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development, Inc. Malignant Neoplasm of Breast August 2017 Phase 1
    NCT02624557 Novartis Pharmaceuticals|Novartis Hepatic Impairment December 21, 2015 Phase 1
    NCT02437318 Novartis Pharmaceuticals|Novartis Breast Cancer July 23, 2015 Phase 3
    NCT03056755 Novartis Pharmaceuticals|Novartis Breast Cancer July 15, 2017 Phase 2
    NCT02620839 Pamela Munster|University of California, San Francisco Solid Tumors December 1, 2016 Phase 1
    NCT02077933 Novartis Pharmaceuticals|Novartis Neoplasms|Breast Neoplasms|Kidney Neoplasms|Pancreatic Neuroendocine Neoplasms May 2014 Phase 1
    NCT02058381 Novartis Pharmaceuticals|Novartis Pre-menopausal Breast Cancer|PI3K Pathway Inhibition May 6, 2014 Phase 1
    NCT02273219 Richard D. Carvajal|Columbia University Uveal Melanoma November 2014 Phase 1
    NCT02051751 Novartis Pharmaceuticals|Novartis Neoplasms, Breast Neoplasms, Head and Neck Neoplasms March 5, 2014 Phase 1
    NCT01219699 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors With an Alteration of the PIK3CA Gene|Estrogen Receptor Positive Breast Cancer October 5, 2010 Phase 1
    NCT01449058 Array BioPharma Advanced and Selected Solid Tumors, AML, High Risk and Very High Risk MDS March 2012 Phase 1|Phase 2
    NCT01623349 Dana-Farber Cancer Institute|Novartis|AstraZeneca Ovarian Cancer|Breast Cancer September 2012 Phase 1
    NCT01791478 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Invasive Ductal Breast Carcinoma|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer April 2013 Phase 1
    NCT02282371 Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals Head and Neck Squamous Cell Cancer October 2014 Phase 1
    NCT01928459 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors|Metastatic Solid Tumors October 2013 Phase 1
    NCT01735968 Novartis Pharmaceuticals|Novartis 3rd Line GIST February 2013 Phase 1
    NCT01870505 Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals Metastatic or Locally-advanced Unresectable Breast Cancer May 2013 Phase 1
    NCT02038010 Northwestern University|Novartis|National Cancer Institute (NCI) HER2-positive Breast Cancer|Recurrent Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer February 2014 Phase 1
    NCT01613950 Novartis Pharmaceuticals|Novartis Stomach Neoplasms Esophageal Neoplasms Metastatic Gastric Cancer Mutated PI3KCA Protein Overexpressed HER2 Protein December 2012 Phase 1
    NCT01387321 Novartis Pharmaceuticals|Novartis Advanced Solid Tumor September 2011 Phase 1
    NCT02167854 Memorial Sloan Kettering Cancer Center|Novartis Breast Cancer June 16, 2014 Phase 1
    NCT02379247 University of Kansas Medical Center|Novartis Pharmaceuticals Breast Cancer February 2015 Phase 1|Phase 2
    NCT01708161 Novartis Pharmaceuticals|NantCell, Inc.|Novartis PIK3CA Mutated Advanced Solid Tumors|PIK3CA Amplified Advanced Solid Tumors November 27, 2012 Phase 1|Phase 2
    NCT02145312 Yonsei University Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck October 2016 Phase 2
    NCT02144038 Novartis Pharmaceuticals|Novartis Relapsed and Refractory Multiple Myeloma July 2014 Phase 1|Phase 2
    NCT02155088 H. Lee Moffitt Cancer Center and Research Institute|Novartis Pancreatic Cancer October 30, 2014 Phase 1
    NCT03138070 Lawson Health Research Institute Head and Neck Squamous Cell Cancer May 2017
    NCT01602315 Novartis Pharmaceuticals|Novartis Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma|Recurrent Head and Neck Squamous Cell Carcinoma|Metastatic Head and Neck Squamous Cell Carcinoma November 2012 Phase 1|Phase 2
    NCT01719380 Array BioPharma Colorectal Cancer November 2012 Phase 1|Phase 2
    NCT02550743 howard safran|Brown University|Lifespan|Novartis Pharmaceuticals Corporation (Financial supporter) Rectal Cancer June 2016 Phase 1
    NCT02537223 University Health Network, Toronto|Novartis Pharmaceuticals Squamous Cell Carcinoma of Head and Neck|Locoregionally Advanced September 2015 Phase 1
    NCT01872260 Novartis Pharmaceuticals|Novartis Breast Cancer October 22, 2013 Phase 1
    NCT01822613 Novartis Pharmaceuticals|Novartis Esophageal Squamous Cell Carcinoma July 26, 2013 Phase 1
    NCT02088684 Novartis Pharmaceuticals|Novartis Breast Cancer May 2014 Phase 1|Phase 2
    NCT01923168 Novartis Pharmaceuticals|Novartis Breast Cancer March 11, 2014 Phase 2
    NCT02734615 Novartis Pharmaceuticals|Novartis Advanced or Metastatic ER+ Breast Cancer April 27, 2016 Phase 1
    NCT02298595 Julie E. Bauman, MD, MPH|Novartis|University of Pittsburgh Carcinoma, Squamous|Squamous Cell Carcinoma|Oropharyngeal Neoplasms|Oropharyngeal Cancer August 2016 Phase 1|Phase 2
    NCT02276027 Novartis Pharmaceuticals|Novartis Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma January 20, 2015 Phase 2
    NCT02506556 Peter MacCallum Cancer Centre, Australia|Novartis Pharmaceuticals Metastatic Breast Cancer July 2015 Phase 2
    NCT01300962 UNC Lineberger Comprehensive Cancer Center|Novartis Pharmaceuticals Metastatic Breast Cancer August 2011 Phase 1
    NCT03207529 M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development, Inc. Malignant Neoplasm of Breast August 2017 Phase 1
    NCT02624557 Novartis Pharmaceuticals|Novartis Hepatic Impairment December 21, 2015 Phase 1
    NCT02437318 Novartis Pharmaceuticals|Novartis Breast Cancer July 23, 2015 Phase 3
    NCT03056755 Novartis Pharmaceuticals|Novartis Breast Cancer July 15, 2017 Phase 2
    NCT02620839 Pamela Munster|University of California, San Francisco Solid Tumors December 1, 2016 Phase 1
    NCT02077933 Novartis Pharmaceuticals|Novartis Neoplasms|Breast Neoplasms|Kidney Neoplasms|Pancreatic Neuroendocine Neoplasms May 2014 Phase 1
    NCT02058381 Novartis Pharmaceuticals|Novartis Pre-menopausal Breast Cancer|PI3K Pathway Inhibition May 6, 2014 Phase 1
    NCT02273219 Richard D. Carvajal|Columbia University Uveal Melanoma November 2014 Phase 1
    NCT02051751 Novartis Pharmaceuticals|Novartis Neoplasms, Breast Neoplasms, Head and Neck Neoplasms March 5, 2014 Phase 1
    NCT01219699 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors With an Alteration of the PIK3CA Gene|Estrogen Receptor Positive Breast Cancer October 5, 2010 Phase 1
    NCT01449058 Array BioPharma Advanced and Selected Solid Tumors, AML, High Risk and Very High Risk MDS March 2012 Phase 1|Phase 2
    NCT01623349 Dana-Farber Cancer Institute|Novartis|AstraZeneca Ovarian Cancer|Breast Cancer September 2012 Phase 1
    NCT01791478 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Invasive Ductal Breast Carcinoma|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer April 2013 Phase 1
    NCT02282371 Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals Head and Neck Squamous Cell Cancer October 2014 Phase 1
    NCT01928459 Novartis Pharmaceuticals|Novartis Advanced Solid Tumors|Metastatic Solid Tumors October 2013 Phase 1
    NCT01735968 Novartis Pharmaceuticals|Novartis 3rd Line GIST February 2013 Phase 1
    NCT01870505 Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals Metastatic or Locally-advanced Unresectable Breast Cancer May 2013 Phase 1
    NCT02038010 Northwestern University|Novartis|National Cancer Institute (NCI) HER2-positive Breast Cancer|Recurrent Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer February 2014 Phase 1
    NCT01613950 Novartis Pharmaceuticals|Novartis Stomach Neoplasms Esophageal Neoplasms Metastatic Gastric Cancer Mutated PI3KCA Protein Overexpressed HER2 Protein December 2012 Phase 1
    NCT01387321 Novartis Pharmaceuticals|Novartis Advanced Solid Tumor September 2011 Phase 1
    NCT02167854 Memorial Sloan Kettering Cancer Center|Novartis Breast Cancer June 16, 2014 Phase 1
    NCT02379247 University of Kansas Medical Center|Novartis Pharmaceuticals Breast Cancer February 2015 Phase 1|Phase 2
    NCT01708161 Novartis Pharmaceuticals|NantCell, Inc.|Novartis PIK3CA Mutated Advanced Solid Tumors|PIK3CA Amplified Advanced Solid Tumors November 27, 2012 Phase 1|Phase 2
    NCT02145312 Yonsei University Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck October 2016 Phase 2
    NCT02144038 Novartis Pharmaceuticals|Novartis Relapsed and Refractory Multiple Myeloma July 2014 Phase 1|Phase 2
    NCT02155088 H. Lee Moffitt Cancer Center and Research Institute|Novartis Pancreatic Cancer October 30, 2014 Phase 1
    NCT03138070 Lawson Health Research Institute Head and Neck Squamous Cell Cancer May 2017
    NCT01602315 Novartis Pharmaceuticals|Novartis Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma|Recurrent Head and Neck Squamous Cell Carcinoma|Metastatic Head and Neck Squamous Cell Carcinoma November 2012 Phase 1|Phase 2
    NCT01719380 Array BioPharma Colorectal Cancer November 2012 Phase 1|Phase 2
    NCT02550743 howard safran|Brown University|Lifespan|Novartis Pharmaceuticals Corporation (Financial supporter) Rectal Cancer June 2016 Phase 1
    NCT02537223 University Health Network, Toronto|Novartis Pharmaceuticals Squamous Cell Carcinoma of Head and Neck|Locoregionally Advanced September 2015 Phase 1
    NCT01872260 Novartis Pharmaceuticals|Novartis Breast Cancer October 22, 2013 Phase 1
    NCT01822613 Novartis Pharmaceuticals|Novartis Esophageal Squamous Cell Carcinoma July 26, 2013 Phase 1
    NCT02088684 Novartis Pharmaceuticals|Novartis Breast Cancer May 2014 Phase 1|Phase 2
    NCT01923168 Novartis Pharmaceuticals|Novartis Breast Cancer March 11, 2014 Phase 2
    NCT02734615 Novartis Pharmaceuticals|Novartis Advanced or Metastatic ER+ Breast Cancer April 27, 2016 Phase 1
    NCT02298595 Julie E. Bauman, MD, MPH|Novartis|University of Pittsburgh Carcinoma, Squamous|Squamous Cell Carcinoma|Oropharyngeal Neoplasms|Oropharyngeal Cancer August 2016 Phase 1|Phase 2
    NCT02276027 Novartis Pharmaceuticals|Novartis Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma January 20, 2015 Phase 2
    NCT02506556 Peter MacCallum Cancer Centre, Australia|Novartis Pharmaceuticals Metastatic Breast Cancer July 2015 Phase 2
    NCT01300962 UNC Lineberger Comprehensive Cancer Center|Novartis Pharmaceuticals Metastatic Breast Cancer August 2011 Phase 1
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.2652 mL 11.3258 mL 22.6516 mL
    5 mM 0.4530 mL 2.2652 mL 4.5303 mL
    10 mM 0.2265 mL 1.1326 mL 2.2652 mL
    Cell Assay
    [3]

    BYL-719 (BYL719) is dissolved in DMSO and stored, and then diluted with appropriate media before use[3].

    Two thousand tumor cells are seeded into 96-well plates and, the day after, the cells are treated with BYL-719 (1-50 µM) for 72 hr. Cell growth/viability is determined using a colorimetric assay using sodium 3′[1-(phenylaminocarbonyl)-3,4-tetrazolium]-bis(4-methoxy-6-nitro-)benzene sulfonic acid hydrate (XTT Reagent Assay Kit). Absorbance is read at 490 nm. Cell viability is also determined by trypan blue exclusion assay; viable and nonviable cells are counted manually after 24 and 48 hr of treatment[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    BYL-719 (NVP-BYL719) is formulated in solution by solving the compound in N-methyl pyrrolidone, polyethylene glycol 300, solutol HS15, and water (10%:30%:20%:40%, v/v) or in suspension in 1% (w/v) carboxymethylcellulose (CMC) + 0.5% (w/v) Tween 80 (Rat)[2].
    BYL-719 (BYL719) is prepared in methylcellulose 0.5% (Mice)[3].

    Rat[2]
    Tumor xenografts are grown subcutaneously or orthotopically in nude mice or nude Rowett rats (Hsd: RH-Fox1rnu) by injection of 3×106 to 1×10 7 cells or implantation of tumor fragments of approximately 50 mg. Tumor-bearing animals mice are treated with either vehicle control, NVP-BYL719, or NVP-BKM120 (p.o., every day) at the doses indicated. For efficacy studies, tumor-bearing animals are enrolled when subcutaneously implanted tumors reached about 200 mm3 and treated with BYL-719 at 50 mg/kg daily. The response is reported as percentage change in tumor volume at last day of treatment relative to day 0 (start of treatment).
    Mice[3]
    A 5-week-old male C57Bl/6J mice are anesthetized by inhalation of an isoflurane/air mixture (2%, 1 L/min) before intramuscular injection of 1×106 mouse MOS-J osteosarcoma cells in close proximity to the tibia, leading to a rapidly growing tumor in soft tissue with secondary contiguous bone invasion. Tumors appeare at the injection site 8 days later and lead to osteoblastic lesions reproducing the osteoblastic form of human osteosarcoma. Three groups (n=6 per group) of C57Bl/6J are assigned randomly to receive either placebo or BYL-719 (oral administration, 12.5-50 mg/kg daily). The preventive treatment starts 1 day after tumor cells inoculation. Four groups of 6 C57Bl/6J are assigned randomly to receive either placebo (oral administration of methylcellulose 0.5% and intraperitoneal injection of water), BYL-719 (oral administration of 50 mg/kg per day), ifosfamide (intraperitoneal injection of 30 mg/kg three times during the first week), or a combination of BYL-719 (50 mg/kg daily) and ifosfamide (30 mg/kg, three times during the first week). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    441.47

    Formula

    C₁₉H₂₂F₃N₅O₂S

    CAS No.

    1217486-61-7

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 40 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.04%

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    Product Name:
    BYL-719
    Cat. No.:
    HY-15244
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