1. PI3K/Akt/mTOR
  2. PI3K

NVP-BKM120 (Synonyms: Buparlisib; BKM120)

Cat. No.: HY-70063 Purity: 99.68%
Data Sheet SDS Handling Instructions

NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively.

For research use only. We do not sell to patients.
NVP-BKM120 Chemical Structure

NVP-BKM120 Chemical Structure

CAS No. : 944396-07-0

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10 mM * 1 mL in DMSO $66 In-stock
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500 mg $450 In-stock
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Customer Review

Other Forms of NVP-BKM120:

    NVP-BKM120 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).

    NVP-BKM120 purchased from MCE. Usage Cited in: PLoS One. 2016 Jan 28;11(1):e0147682.

    CHP-212 and SK-N-AS cells are treated with indicated concentrations of AZD6244, MEK162, Everolimus or AZD8055 or combinations thereof as indicated for 1 hour. Then, cells are lysed and analysed by Western blot. Phosphorylation levels of AKT, ERK and S6 are detected by specific anti-phospho antibodies. Loading is verified by specific antibodies to total AKT, ERK and anti-tubulin.

    NVP-BKM120 purchased from MCE. Usage Cited in: Nat Med. 2016 Jul;22(7):723-6.

    Selective response of HER2-positive PDX DF-BM355 to the combination of BKM120/RAD001. Western blot analysis of lysates from vehicle-treated or BKM120-treated DF-BM355 in vivo.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively.

    IC50 & Target

    IC50: 52 nM (p110α), 166 nM (p110β), 116 nM (p110δ), 262 nM (p110γ)[1]

    In Vitro

    NVP-BKM120 (BKM120) exhibits 50-300 nM activity for class I PI3K’s, including the most common p110α mutants. Additionally, NVP-BKM120 exhibits lower potency against class III and class IV PI3K's, where 2, 5, >5, and >25 μM biochemical activity is observed for inhibition of VPS34, mTOR, DNAPK, and PI4K, respectively[1]. NVP-BKM120 induces multiple myeloma (MM) cell apoptosis in both dose- and time-dependent manners. NVP-BKM120 at concentrations ≥10 μM induces significant apoptosis in all tested MM cell lines at 24 h (P<0.05, compares with control). Therefore, 10 μM NVP-BKM120 and 24-h treatment are chose in in the following experiments if not stated otherwise. NVP-BKM120 treatment results in a dose-dependent growth inhibition in all tested MM cell lines. NVP-BKM120 IC50 varies among tested MM cells. At 24 h treatment, IC50 for ARP-1, ARK, and MM.1R is between 1 and 10 μM, while IC50 for MM.1S is <1 μM, and IC50 for U266 is between 10 and 100 μM. In summary, NVP-BKM120 treatment results in MM cell growth inhibition and apoptosis in dose- and time-dependent manners[2].

    In Vivo

    In A2780 xenograft tumors, oral dosing of NVP-BKM120 (BKM120) at 3, 10, 30, 60, and 100 mg/kg results in a dose dependent modulation of pAKTSer473. Partial inhibition of pAKTSer473 is observed at 3 and 10 mg/kg, and near complete inhibition is observed at doses of 30, 60, or 100 mg/kg, respectively. Inhibition of pAKT (normalized to total AKT) tracked well with both plasma and tumor drug exposure[1]. Mice receiving NVP-BKM120 (5 μM per kg per day for 15 days) treatment has significantly smaller tumor burdens as compare with control mice, which are measured as tumor volume (P<0.05) and level of circulating human kappa chain (P<0.05). In addition, NVP-BKM120 treatment significantly prolongs the survival of tumor-bearing mice (P<0.05)[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT02035124 SCRI Development Innovations, LLC|Novartis Advanced Prostate Cancer April 2014 Phase 2
    NCT01248494 Vanderbilt-Ingram Cancer Center Metastatic Breast Cancer November 2010 Phase 1
    NCT01283048 Toni Choueiri, MD|Beth Israel Deaconess Medical Center|Dana-Farber Cancer Institute Renal Cell Carcinoma September 2011 Phase 1
    NCT02128724 University of Oxford|Cancer Research UK|Novartis Carcinoma, Non-Small-Cell Lung April 2013 Phase 1
    NCT01570296 National Cancer Centre, Singapore|Novartis Non-Small Cell Lung Cancer|Solid Tumors October 2011 Phase 1
    NCT01550380 University of Utah|Novartis Endometrial Cancer May 2014 Phase 2
    NCT01513356 Sofia Perea, Director Clinical Trials Unit.|Novartis|Grupo Hospital de Madrid Breast Cancer October 2012 Early Phase 1
    NCT01487265 SCRI Development Innovations, LLC|Novartis Non Small Cell Lung Cancer March 2014 Phase 2
    NCT01527877 Yonsei University Head Neck Cancer Squamous Cell Metastatic|Head Neck Cancer Squamous Cell Recurrent September 2012 Phase 2
    NCT01385293 Andrew J. Armstrong, MD|Novartis Pharmaceuticals|Duke University Prostate Cancer|Metastatic (Spread to Other Areas of the Body) August 2011 Phase 2
    NCT01589861 Institut Paoli-Calmettes Breast Cancer December 2011 Phase 1|Phase 2
    NCT01695473 Charles Ryan|Novartis|University of California, San Francisco High Risk Prostate Cancer October 2012 Phase 2
    NCT02487823 Institut Paoli-Calmettes|Novartis Non Castrate Metastatic Prostate Cancer October 2014 Phase 1
    NCT01830504 Hospices Civils de Lyon Thyroid Cancers April 2013 Phase 2
    NCT02439489 Fondazione Michelangelo Solid Tumors December 2012 Phase 1
    NCT01833169 Novartis Pharmaceuticals|Novartis PI3K Pathway Activated Tumors March 2013 Phase 2
    NCT01396499 M.D. Anderson Cancer Center|Novartis Leukemia July 2012 Phase 1
    NCT02113878 Dana-Farber Cancer Institute|Novartis Pharmaceuticals Carcinoma, Squamous Cell of Head and Neck|HPV Positive Oropharyngeal Squamous Cell Carcinoma|Hypopharyngeal Cancer|Early Invasive Cervical Squamous Cell Carcinoma|Carcinoma of Larynx|Cancer of Nasopharynx October 2014 Phase 1
    NCT01571024 UNC Lineberger Comprehensive Cancer Center Advanced Solid Tumors|Metastatic Colorectal Cancer|Metastatic Pancreatic Cancer May 2012 Phase 1
    NCT01806649 Prince of Songkla University Esophageal Cancer January 2013 Phase 2
    NCT01304602 University of Kansas Medical Center Colorectal Cancer February 2011 Phase 1
    NCT01623349 Dana-Farber Cancer Institute|Novartis|AstraZeneca Ovarian Cancer|Breast Cancer September 2012 Phase 1
    NCT02301364 Memorial Sloan Kettering Cancer Center|Novartis Lymphoma|Primary Central Nervous System Lymphoma|Recurrent/Refractory Secondary Central Nervous System Lymphoma November 20, 2014 Phase 2
    NCT01068483 Novartis Pharmaceuticals|Novartis Breast Cancer|Colon Cancer|Ovarian Cancer|Endometrium Cancer November 2008 Phase 1
    NCT01349660 SCRI Development Innovations, LLC|Novartis Glioblastoma Multiforme December 2011 Phase 1|Phase 2
    NCT01953445 Washington University School of Medicine Breast Neoplasms August 2014 Phase 2
    NCT01468688 Novartis Pharmaceuticals|Novartis 3rd Line GIST April 20, 2012 Phase 1
    NCT01790932 Dana-Farber Cancer Institute Breast Cancer February 2013 Phase 2
    NCT01613677 Novartis Pharmaceuticals|Novartis Treatment for Metastatic or Locally Advanced Cervical Cancer November 2015 Phase 2
    NCT01629615 SOLTI Breast Cancer Research Group|Novartis Pharmaceuticals|Dana-Farber Cancer Institute|Stand Up To Cancer Breast Cancer June 2012 Phase 2
    NCT01737450 Centre Leon Berard|National Cancer Institute, France|Fondation ARC Head and Neck Neoplasms|Neoplasm Metastasis|Recurrent Disease|Progressive Disease January 2013 Phase 2
    NCT01297491 Novartis Pharmaceuticals|Novartis Non-small Cell Lung Cancer May 2011 Phase 2
    NCT01473901 Novartis Pharmaceuticals|Novartis Glioblastoma December 30, 2011 Phase 1
    NCT01591421 Canadian Cancer Trials Group Metastatic Colorectal Cancer May 1, 2012 Phase 1|Phase 2
    NCT02194049 University of California, Davis|Novartis Extensive Stage Small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific July 2014 Phase 1
    NCT02404844 University Hospital, Essen|iOMEDICO AG|Novartis Pharmaceuticals Breast Cancer December 2014 Phase 2
    NCT01626209 Novartis Pharmaceuticals|Novartis Advanced Breast Cancer, Advanced Carcinomas With Squamous Cell Histology July 2012 Phase 1
    NCT01297452 Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals|Sai Life Sciences Solid Tumors February 15, 2011 Phase 1
    NCT01470209 Emory University|Novartis Pharmaceuticals Solid Tumors|Lung Cancer January 2012 Phase 1
    NCT01339052 Patrick Y. Wen, MD|Brigham and Women's Hospital|Massachusetts General Hospital|Novartis Pharmaceuticals|M.D. Anderson Cancer Center|Memorial Sloan Kettering Cancer Center|University of California, San Francisco|University of California, Los Angeles|University of Utah|Dana-Farber Cancer Institute Glioblastoma September 2011 Phase 2
    NCT01633060 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer October 3, 2012 Phase 3
    NCT02049541 Kami Maddocks|Novartis|Ohio State University Comprehensive Cancer Center Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Splenic Marginal Zone Lymphoma|Waldenström Macroglobulinemia July 2014 Phase 1
    NCT01572727 Novartis Pharmaceuticals|Novartis Breast Cancer August 2012 Phase 2|Phase 3
    NCT01283503 Novartis Pharmaceuticals|Novartis Advanced Solid Tumor October 2009 Phase 1
    NCT01155453 Novartis Pharmaceuticals|Novartis Advanced and Selected Solid Tumors April 2010 Phase 1
    NCT01540253 Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis Unspecified Adult Solid Tumor, Protocol Specific May 2012 Phase 1
    NCT01289041 Novartis Pharmaceuticals|Novartis Advanced Endometrial Cancer February 2011 Phase 2
    NCT02000882 US Oncology Research|Novartis Pharmaceuticals Brain Metastases|Breast Cancer|Metastatic Breast Cancer May 29, 2014 Phase 2
    NCT01363232 Array BioPharma Advanced Solid Tumors|Selected Solid Tumors August 2011 Phase 1
    NCT01693614 Novartis Pharmaceuticals|Novartis Diffuse Large B-cell Lymphoma, Mantle Cell Lymphoma, Follicular Lymphoma February 28, 2013 Phase 2
    NCT01610284 Novartis Pharmaceuticals|Novartis Breast Cancer August 7, 2012 Phase 3
    NCT01723800 City of Hope Medical Center|National Cancer Institute (NCI) Recurrent Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer July 2013 Phase 1
    NCT02220855 Patrick Joseph Loehrer Sr.|Novartis Pharmaceuticals|Indiana University Thymoma September 2014 Phase 2
    NCT01741753 Dana-Farber Cancer Institute Prostate Cancer November 2012 Phase 1
    NCT01634061 Novartis Pharmaceuticals|Novartis Castration-resistant Prostate Cancer September 2012 Phase 1
    NCT01512251 University of California, San Francisco|Novartis BRAF Mutant Metastatic Melanoma June 2012 Phase 1|Phase 2
    NCT01339442 Washington University School of Medicine|National Cancer Institute (NCI) Estrogen Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer November 14, 2011 Phase 1
    NCT01576666 Novartis Pharmaceuticals|Novartis Dose Escalation|Safety|Preliminary Efficacy|Advanced Solid Tumors|Metastatic Breast Cancer|Advanced Pancreatic Adenocarcinoma|Metastatic Colorectal Cancer|Recurrent Glioblastoma Multiforme|Gastric Cancer|Gastroesophageal Junction Cancer|Triple Negative Metastatic Breast Cancer|Hormone Receptor Positive (ER+/PR+, and Her2-) Metastatic Breast Cancer July 2012 Phase 1
    NCT01816594 Novartis Pharmaceuticals|Breast International Group|German Breast Group (GBG)|SOLTI Breast Cancer Research Group|Novartis HER2-positive, Newly Diagnosed, Primary Breast Cancer, Neoadjuvant Therapy, Trastuzumab September 2013 Phase 2
    NCT01501604 Massachusetts General Hospital|Novartis Pharmaceuticals Lung Cancer|Breast Cancer|Colorectal Cancer|Cholangiocarcinoma|Solid Tumors January 2012 Phase 2
    NCT01816984 University of Chicago|National Cancer Institute (NCI) Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primary|Recurrent Salivary Gland Cancer|Recurrent Squamous Cell Carcinoma of the Hypopharynx|Recurrent Squamous Cell Carcinoma of the Larynx|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity|Recurrent Squamous Cell Carcinoma of the Nasopharynx|Recurrent Squamous Cell Carcinoma of the Oropharynx|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Na May 2013 Phase 1|Phase 2
    NCT02117817 Rutgers, The State University of New Jersey|Rutgers Cancer Institute of New Jersey|National Cancer Institute (NCI) Ovarian Cancer|Endometrial Cancer|Recurrent Ovarian Cancer|Recurrent Endometrial Cancer February 2015 Phase 1
    NCT01727128 Novartis Pharmaceuticals|Novartis Hepatic Impairment October 2011 Phase 1
    NCT02088684 Novartis Pharmaceuticals|Novartis Breast Cancer May 2014 Phase 1|Phase 2
    NCT01397877 ARCAGY/ GINECO GROUP Endometrial Cancer December 2011 Phase 2
    NCT01285466 Novartis Pharmaceuticals|Novartis Metastatic or Locally Advanced Solid Tumors January 2011 Phase 1
    NCT01132664 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer|HER2+ Breast Cancer May 2010 Phase 1|Phase 2
    NCT01730248 Novartis Pharmaceuticals|Incyte Corporation|Novartis Myelofibrosis December 18, 2012 Phase 1
    NCT02058381 Novartis Pharmaceuticals|Novartis Pre-menopausal Breast Cancer|PI3K Pathway Inhibition May 6, 2014 Phase 1
    NCT01923168 Novartis Pharmaceuticals|Novartis Breast Cancer March 11, 2014 Phase 2
    NCT02159066 Array BioPharma Melanoma July 2014 Phase 2
    NCT02035124 SCRI Development Innovations, LLC|Novartis Advanced Prostate Cancer April 2014 Phase 2
    NCT01248494 Vanderbilt-Ingram Cancer Center Metastatic Breast Cancer November 2010 Phase 1
    NCT01283048 Toni Choueiri, MD|Beth Israel Deaconess Medical Center|Dana-Farber Cancer Institute Renal Cell Carcinoma September 2011 Phase 1
    NCT02128724 University of Oxford|Cancer Research UK|Novartis Carcinoma, Non-Small-Cell Lung April 2013 Phase 1
    NCT01570296 National Cancer Centre, Singapore|Novartis Non-Small Cell Lung Cancer|Solid Tumors October 2011 Phase 1
    NCT01550380 University of Utah|Novartis Endometrial Cancer May 2014 Phase 2
    NCT01513356 Sofia Perea, Director Clinical Trials Unit.|Novartis|Grupo Hospital de Madrid Breast Cancer October 2012 Early Phase 1
    NCT01487265 SCRI Development Innovations, LLC|Novartis Non Small Cell Lung Cancer March 2014 Phase 2
    NCT01527877 Yonsei University Head Neck Cancer Squamous Cell Metastatic|Head Neck Cancer Squamous Cell Recurrent September 2012 Phase 2
    NCT01385293 Andrew J. Armstrong, MD|Novartis Pharmaceuticals|Duke University Prostate Cancer|Metastatic (Spread to Other Areas of the Body) August 2011 Phase 2
    NCT01589861 Institut Paoli-Calmettes Breast Cancer December 2011 Phase 1|Phase 2
    NCT01695473 Charles Ryan|Novartis|University of California, San Francisco High Risk Prostate Cancer October 2012 Phase 2
    NCT02487823 Institut Paoli-Calmettes|Novartis Non Castrate Metastatic Prostate Cancer October 2014 Phase 1
    NCT01830504 Hospices Civils de Lyon Thyroid Cancers April 2013 Phase 2
    NCT02439489 Fondazione Michelangelo Solid Tumors December 2012 Phase 1
    NCT01833169 Novartis Pharmaceuticals|Novartis PI3K Pathway Activated Tumors March 2013 Phase 2
    NCT01396499 M.D. Anderson Cancer Center|Novartis Leukemia July 2012 Phase 1
    NCT02113878 Dana-Farber Cancer Institute|Novartis Pharmaceuticals Carcinoma, Squamous Cell of Head and Neck|HPV Positive Oropharyngeal Squamous Cell Carcinoma|Hypopharyngeal Cancer|Early Invasive Cervical Squamous Cell Carcinoma|Carcinoma of Larynx|Cancer of Nasopharynx October 2014 Phase 1
    NCT01571024 UNC Lineberger Comprehensive Cancer Center Advanced Solid Tumors|Metastatic Colorectal Cancer|Metastatic Pancreatic Cancer May 2012 Phase 1
    NCT01806649 Prince of Songkla University Esophageal Cancer January 2013 Phase 2
    NCT01304602 University of Kansas Medical Center Colorectal Cancer February 2011 Phase 1
    NCT01623349 Dana-Farber Cancer Institute|Novartis|AstraZeneca Ovarian Cancer|Breast Cancer September 2012 Phase 1
    NCT02301364 Memorial Sloan Kettering Cancer Center|Novartis Lymphoma|Primary Central Nervous System Lymphoma|Recurrent/Refractory Secondary Central Nervous System Lymphoma November 20, 2014 Phase 2
    NCT01068483 Novartis Pharmaceuticals|Novartis Breast Cancer|Colon Cancer|Ovarian Cancer|Endometrium Cancer November 2008 Phase 1
    NCT01349660 SCRI Development Innovations, LLC|Novartis Glioblastoma Multiforme December 2011 Phase 1|Phase 2
    NCT01953445 Washington University School of Medicine Breast Neoplasms August 2014 Phase 2
    NCT01468688 Novartis Pharmaceuticals|Novartis 3rd Line GIST April 20, 2012 Phase 1
    NCT01790932 Dana-Farber Cancer Institute Breast Cancer February 2013 Phase 2
    NCT01613677 Novartis Pharmaceuticals|Novartis Treatment for Metastatic or Locally Advanced Cervical Cancer November 2015 Phase 2
    NCT01629615 SOLTI Breast Cancer Research Group|Novartis Pharmaceuticals|Dana-Farber Cancer Institute|Stand Up To Cancer Breast Cancer June 2012 Phase 2
    NCT01737450 Centre Leon Berard|National Cancer Institute, France|Fondation ARC Head and Neck Neoplasms|Neoplasm Metastasis|Recurrent Disease|Progressive Disease January 2013 Phase 2
    NCT01297491 Novartis Pharmaceuticals|Novartis Non-small Cell Lung Cancer May 2011 Phase 2
    NCT01473901 Novartis Pharmaceuticals|Novartis Glioblastoma December 30, 2011 Phase 1
    NCT01591421 Canadian Cancer Trials Group Metastatic Colorectal Cancer May 1, 2012 Phase 1|Phase 2
    NCT02194049 University of California, Davis|Novartis Extensive Stage Small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific July 2014 Phase 1
    NCT02404844 University Hospital, Essen|iOMEDICO AG|Novartis Pharmaceuticals Breast Cancer December 2014 Phase 2
    NCT01626209 Novartis Pharmaceuticals|Novartis Advanced Breast Cancer, Advanced Carcinomas With Squamous Cell Histology July 2012 Phase 1
    NCT01297452 Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals|Sai Life Sciences Solid Tumors February 15, 2011 Phase 1
    NCT01470209 Emory University|Novartis Pharmaceuticals Solid Tumors|Lung Cancer January 2012 Phase 1
    NCT01339052 Patrick Y. Wen, MD|Brigham and Women's Hospital|Massachusetts General Hospital|Novartis Pharmaceuticals|M.D. Anderson Cancer Center|Memorial Sloan Kettering Cancer Center|University of California, San Francisco|University of California, Los Angeles|University of Utah|Dana-Farber Cancer Institute Glioblastoma September 2011 Phase 2
    NCT01633060 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer October 3, 2012 Phase 3
    NCT02049541 Kami Maddocks|Novartis|Ohio State University Comprehensive Cancer Center Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Splenic Marginal Zone Lymphoma|Waldenström Macroglobulinemia July 2014 Phase 1
    NCT01572727 Novartis Pharmaceuticals|Novartis Breast Cancer August 2012 Phase 2|Phase 3
    NCT01283503 Novartis Pharmaceuticals|Novartis Advanced Solid Tumor October 2009 Phase 1
    NCT01155453 Novartis Pharmaceuticals|Novartis Advanced and Selected Solid Tumors April 2010 Phase 1
    NCT01540253 Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis Unspecified Adult Solid Tumor, Protocol Specific May 2012 Phase 1
    NCT01289041 Novartis Pharmaceuticals|Novartis Advanced Endometrial Cancer February 2011 Phase 2
    NCT02000882 US Oncology Research|Novartis Pharmaceuticals Brain Metastases|Breast Cancer|Metastatic Breast Cancer May 29, 2014 Phase 2
    NCT01363232 Array BioPharma Advanced Solid Tumors|Selected Solid Tumors August 2011 Phase 1
    NCT01693614 Novartis Pharmaceuticals|Novartis Diffuse Large B-cell Lymphoma, Mantle Cell Lymphoma, Follicular Lymphoma February 28, 2013 Phase 2
    NCT01610284 Novartis Pharmaceuticals|Novartis Breast Cancer August 7, 2012 Phase 3
    NCT01723800 City of Hope Medical Center|National Cancer Institute (NCI) Recurrent Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer July 2013 Phase 1
    NCT02220855 Patrick Joseph Loehrer Sr.|Novartis Pharmaceuticals|Indiana University Thymoma September 2014 Phase 2
    NCT01741753 Dana-Farber Cancer Institute Prostate Cancer November 2012 Phase 1
    NCT01634061 Novartis Pharmaceuticals|Novartis Castration-resistant Prostate Cancer September 2012 Phase 1
    NCT01512251 University of California, San Francisco|Novartis BRAF Mutant Metastatic Melanoma June 2012 Phase 1|Phase 2
    NCT01339442 Washington University School of Medicine|National Cancer Institute (NCI) Estrogen Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer November 14, 2011 Phase 1
    NCT01576666 Novartis Pharmaceuticals|Novartis Dose Escalation|Safety|Preliminary Efficacy|Advanced Solid Tumors|Metastatic Breast Cancer|Advanced Pancreatic Adenocarcinoma|Metastatic Colorectal Cancer|Recurrent Glioblastoma Multiforme|Gastric Cancer|Gastroesophageal Junction Cancer|Triple Negative Metastatic Breast Cancer|Hormone Receptor Positive (ER+/PR+, and Her2-) Metastatic Breast Cancer July 2012 Phase 1
    NCT01816594 Novartis Pharmaceuticals|Breast International Group|German Breast Group (GBG)|SOLTI Breast Cancer Research Group|Novartis HER2-positive, Newly Diagnosed, Primary Breast Cancer, Neoadjuvant Therapy, Trastuzumab September 2013 Phase 2
    NCT01501604 Massachusetts General Hospital|Novartis Pharmaceuticals Lung Cancer|Breast Cancer|Colorectal Cancer|Cholangiocarcinoma|Solid Tumors January 2012 Phase 2
    NCT01816984 University of Chicago|National Cancer Institute (NCI) Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primary|Recurrent Salivary Gland Cancer|Recurrent Squamous Cell Carcinoma of the Hypopharynx|Recurrent Squamous Cell Carcinoma of the Larynx|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity|Recurrent Squamous Cell Carcinoma of the Nasopharynx|Recurrent Squamous Cell Carcinoma of the Oropharynx|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Na May 2013 Phase 1|Phase 2
    NCT02117817 Rutgers, The State University of New Jersey|Rutgers Cancer Institute of New Jersey|National Cancer Institute (NCI) Ovarian Cancer|Endometrial Cancer|Recurrent Ovarian Cancer|Recurrent Endometrial Cancer February 2015 Phase 1
    NCT01727128 Novartis Pharmaceuticals|Novartis Hepatic Impairment October 2011 Phase 1
    NCT02088684 Novartis Pharmaceuticals|Novartis Breast Cancer May 2014 Phase 1|Phase 2
    NCT01397877 ARCAGY/ GINECO GROUP Endometrial Cancer December 2011 Phase 2
    NCT01285466 Novartis Pharmaceuticals|Novartis Metastatic or Locally Advanced Solid Tumors January 2011 Phase 1
    NCT01132664 Novartis Pharmaceuticals|Novartis Metastatic Breast Cancer|HER2+ Breast Cancer May 2010 Phase 1|Phase 2
    NCT01730248 Novartis Pharmaceuticals|Incyte Corporation|Novartis Myelofibrosis December 18, 2012 Phase 1
    NCT02058381 Novartis Pharmaceuticals|Novartis Pre-menopausal Breast Cancer|PI3K Pathway Inhibition May 6, 2014 Phase 1
    NCT01923168 Novartis Pharmaceuticals|Novartis Breast Cancer March 11, 2014 Phase 2
    NCT02159066 Array BioPharma Melanoma July 2014 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.4367 mL 12.1835 mL 24.3671 mL
    5 mM 0.4873 mL 2.4367 mL 4.8734 mL
    10 mM 0.2437 mL 1.2184 mL 2.4367 mL
    Kinase Assay
    [1]

    NVP-BKM120 to be tested is dissolved in DMSO and directly distributed into a black 384-well plate at 1.25 μL per well. To start the reaction, 25 μL of 10 nM PI3 kinase and 5 μg/mL 1-alpha-phosphatidylinositol (PI) in assay buffer (10 mM Tris pH 7.5, 5 mM MgCl2, 20 mM NaCl, 1 mM DTT and 0.05% CHAPS) are added into each well followed by 25 μL of 2 μM ATP in assay buffer. The reaction is performed until approx 50% of the ATP is depleted, and then stopped by the addition of 25 μL of KinaseGlo solution. The stopped reaction is incubated for 5 minutes and the remaining ATP is then detected via luminescence[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    NVP-BKM120 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    A2780 cells are cultured in DMEM supplemented with 10% FBS. L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 1000 cells per well, 100 uL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. NVP-BKM120 supplied in DMSO (20 mM) are diluted further into DMSO (7.5 uL of 20 mM NVP-BKM120 in 22.5 uL DMSO. Mix well, transfer 10 uL to 20 uL DMSO, repeat until 9 concentrations have been made). The diluted NVP-BKM120 solution (2 uL), is then added to cell medium (500 uL) cell medium. Equal volumes of this solution (100 uL) are added to the cells in 96 well plates and incubated at 37ºC for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    NVP-BKM120 is dissolved in DMSO/PBS (Mice)[2].

    Mice[2]
    Six- to eight-week-old female severe combined immunodeficiency (SCID) mice are used. SCID mice are subcutaneously inoculated in the right flank with 1 million ARP-1 or MM.1S cells suspended in 50 μL phosphate-buffered saline (PBS). After palpable tumor developed (tumor diameter ≥5 mm), mice are treated with intraperitoneal injection of DMSO/PBS or NVP-BKM120 (5 μM per kg per day) for 15 days. Tumor sizes are measured every 5 days, and blood samples are collected at the same period. Tumor burdens are evaluated by measuring tumor size and detecting circulating human kappa chain or lambda chain. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    410.39

    Formula

    C₁₈H₂₁F₃N₆O₂

    CAS No.

    944396-07-0

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    NVP-BKM120 (BKM120) is dissolved in 10% NMP with 90% PEG300[3].

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

    References

    Purity: 99.68%

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