1. PI3K/Akt/mTOR
  2. PI3K

NVP-BKM120 Hydrochloride (Synonyms: BKM-120 hydrochloride; BKM120 hydrochloride; BKM 120 hydrochloride)

Cat. No.: HY-15180 Purity: 98.01%
Data Sheet SDS Handling Instructions

NVP-BKM120 Hcl(BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ.

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

NVP-BKM120 Hydrochloride Chemical Structure

CAS No. : 1312445-63-8

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10 mM * 1 mL in DMSO $66 In-stock
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50 mg $150 In-stock
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NVP-BKM120 Hcl(BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. IC50 value: 52 nM/166 nM/116 nM/262 nM(p110α/β/δ/γ) [1] Target: p110α/β/δ/γ in vitro: BKM120 is not sensitive to Class III and Class IV PI3K's or PI4K. NVP-BKM120 shows great antiproliferation activity to PI3K deregulated cell lines including A2780, U87MG, MCF7 and DU145 with GI50 of 0.1-0.7 nM [1]. BKM120 induces multiple myeloma cells (ARP1, ARK, MM.1S, MM1.R and U266) apoptosis, which results in increased G1-phase cells and decreased S-phase cells. BKM120 induced CD138+ primary MM cell apoptosis and has significant lower cytotoxicity toward CD138? stromal cells. BKM120 exposure could cause upregulation of BimS and downregulation of XIAP [2]. BKM120 demonstrates antiproliferative activity in human gastric cancer cell lines by decreasing mTOR downstream signaling. BKM120 could increase either p-ERK or p-STAT3 in KRAS mutant gastric cancer cells. Combination with STAT3 blockade, BKM120 shows a synergism in cells harboring mutated KRAS by inducing apoptosis, but not in KRAS wild-type cells [3]. in vivo: BKM120 completely inhibits pAktser473 in A2780 xenograft tumors at doses of 30, 60, or 100 mg/kg, respectively. BKM120 also shows antitumor activity against U87MG glioma model at doses of 30 and 60 mg/kg [1]. BKM120 treatment results in significantly reduced tumor volume and level of circulating human kappa chain at 5 μM/kg/day?1in ARP1 SCID mouse model, with prolonged survival [2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
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 19, 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
NCT01248494 Vanderbilt-Ingram Cancer Center Metastatic Breast Cancer November 2010 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 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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Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

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

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NVP-BKM120 Hydrochloride
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