BKM120 (NVP-BKM120, Buparlisib)

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. 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

Customer Reviews(3)

Quality Control & MSDS

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

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Product Description

Biological Activity

Description 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. Phase 2.
Targets p110α [1] p110δ [1] p110β [1] p110γ [1] Vps34 [1]

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IC50 52 nM 116 nM 166 nM 262 nM 2.4 μM
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]
Features

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.).
Solubility 15% Captisol, pH 4, 6 mg/mL
* 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.

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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

References

[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 2014-09-20)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01613677 Not yet recruiting Treatment for Metastatic or Locally Advanced Cervical Cancer Novartis Pharmaceuticals|Novartis July 2015 Phase 2
NCT01971489 Not yet recruiting Recurrent Non-small Cell Lung Cancer|Stage IIIA Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cance  ...more Recurrent Non-small Cell Lung Cancer|Stage IIIA Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific Roswell Park Cancer Institute|National Cancer Institute (  ...more Roswell Park Cancer Institute|National Cancer Institute (NCI) October 2014 Phase 1
NCT02220855 Not yet recruiting Thymoma Indiana University|Novartis Pharmaceuticals September 2014 Phase 2
NCT01953445 Recruiting Breast Neoplasms Washington University School of Medicine August 2014 Phase 2
NCT02049541 Recruiting Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Grade 1 Follicular Lymp  ...more 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 Kami Maddocks|Novartis|Ohio State University Comprehensiv  ...more Kami Maddocks|Novartis|Ohio State University Comprehensive Cancer Center July 2014 Phase 1

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Chemical Information

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

C18H21F3N6O2

CAS No. 944396-07-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 82 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol 2 mg/mL (4 mM)
In vivo 15% Captisol, pH 4 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

Research Area

Customer Reviews (3)


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Rating
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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Rating
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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Rating
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 Citations (18)

Tech Support & FAQs

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