BKM120 (NVP-BKM120, Buparlisib)

BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.

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BKM120 (NVP-BKM120, Buparlisib) Chemical Structure

BKM120 (NVP-BKM120, Buparlisib) Chemical Structure
Molecular Weight: 410.39

Validation & Quality Control

Product Use Citation(34)

Customer Product Validation(3)

Quality Control & MSDS

Related Compound Libraries

BKM120 (NVP-BKM120, Buparlisib) is available in the following compound libraries:

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Product Information

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  • BKM120 (NVP-BKM120, Buparlisib) Mechanism

Product Description

Biological Activity

Description BKM120 (NVP-BKM120, Buparlisib) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 2.
Targets p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)

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IC50 52 nM 116 nM 166 nM 262 nM
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] A recent study shows that BKM120 shows differential forms of cell death on the basis of p53 status of the cells with p53 wild-type cells undergoing apoptotic cell death and p53 mutant/deleted cells having a mitotic catastrophe cell death. BKM120 mediates mitotic catastrophe mainly through Aurora B kinase. [4]
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]

Protocol(Only for Reference)

Kinase Assay: [1]

PI3K biochemical assay (ATP depletion assay) BKM120 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-α-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.
PI3K biochemical assay (filter binding assay) 50 µL/well of a 1:1 mixture of 100 µL/mL L-α-phosphatidylinositol and L-α-phosphatidylserine dissolved in chloroform:ethanol (2.2:7.8) is pipetted into 96-well MaxiSorpTM plates. The solvents are evaporated at room temperature and plates are wa

Cell Assay: [1]

Cell lines A2780 cells.
Concentrations 0-6.6 μM
Incubation Time 3 days.
Method 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 103 cells per well, 100 μL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. BKM120 supplied in DMSO (20 mM) is diluted. The diluted BKM120 solution (2 μL), is then added to cell medium (500 μL) cell medium (concentration from 0-6.6 μM). Equal volumes of this solution (100 μL) are added to the cells in 96 well plates and incubated at 37 °C for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux.

Animal Study: [1]

Animal Models U87MG and A2780 xenografts are established in female nu/nu mice.
Formulation In 15% Captisol.
Dosages ~60 mg/kg.
Administration Dosed orally daily (q.d.).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Burger MT, et al. ACS Med Chem Lett, 2011, 2 (10), 774–779.

[2] Zheng Y, et al. J Mol Med (Berl), 2011 Dec 30.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-08-29)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT01613677 Not yet recruiting Treatment for Metastatic or Locally Advanced Cervical Cancer Novartis Pharmaceuticals|Novartis November 2015 Phase 2
NCT01971489 Withdrawn Adult Solid Neoplasm|Recurrent Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV N  ...more Adult Solid Neoplasm|Recurrent Non-Small Cell Lung Carcinoma|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IV Non-Small Cell Lung Cancer Roswell Park Cancer Institute|National Cancer Institute (  ...more Roswell Park Cancer Institute|National Cancer Institute (NCI) September 2015 Phase 1
NCT02452294 Recruiting Malignant Melanoma|Metastases University Hospital Tuebingen|University Hospital Dresden July 2015 Phase 2
NCT02117817 Withdrawn Ovarian Cancer|Endometrial Cancer|Recurrent Ovarian Cancer|Recurrent Endometrial Cancer Rutgers, The State University of New Jersey|Rutgers Cance  ...more Rutgers, The State University of New Jersey|Rutgers Cancer Institute of New Jersey|National Cancer Institute (NCI) February 2015 Phase 1
NCT02303041 Recruiting Basal Cell Carcinoma of the Skin|Nevoid Basal Cell Carcinoma Syndrome|Recurrent Skin Cancer Stanford University|National Cancer Institute (NCI) February 2015 --

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Chemical Information

Download BKM120 (NVP-BKM120, Buparlisib) SDF
Molecular Weight (MW) 410.39


CAS No. 944396-07-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 82 mg/mL (199.8 mM)
Ethanol 2 mg/mL (4.87 mM)
Water <1 mg/mL (<1 mM)
In vivo 0.5% CMC Na 6 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine

Customer Product Validation (3)

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Source Dr. Zhang of Tianjin Medical University. BKM120 (NVP-BKM120, Buparlisib) purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-10 μM
Incubation Time 3 h
Results BKM120 treatment resulted in a reduction of Akt-308 phosphorylation in A549 cells.

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Source One customer. BKM120 (NVP-BKM120, Buparlisib) purchased from Selleck
Method Cell growth inhibition assay
Cell Lines Melanoma cell lines
Concentrations 0.00000512-10 μM
Incubation Time 72 h
Results BKM120 treatment inhibited Melanoma cells growth in a does-dependent manner.

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Source Dr. Pilar Eroles of INCLIVA Biomedical Research Institute.. BKM120 (NVP-BKM120, Buparlisib) purchased from Selleck
Method MTT assay
Cell Lines JIMT-1 cells
Concentrations 1-1000 nM
Incubation Time 48 h
Results JIMT-1 cells were seeded in 96 well plates (8x10<SUP>3</SUP>cells per well) andtreated with medium containing DMSO as a control and inhibitor BKM-120 (1nM, 5nM, 10nM, 50nM, 100nM, 500nM, 1000nM). Cell growth was measured after 48 hours by MTT assay.Results are expressed as a percent over DMSO control.

Product Use Citation (34)

Tech Support & FAQs

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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