1. PI3K/Akt/mTOR
    Apoptosis
  2. PI3K
    Apoptosis
  3. Buparlisib

Buparlisib (Synonyms: NVP-BKM120; BKM120)

Cat. No.: HY-70063 Purity: 99.90%
Handling Instructions

Buparlisib (NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

For research use only. We do not sell to patients.

Buparlisib Chemical Structure

Buparlisib Chemical Structure

CAS No. : 944396-07-0

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10 mM * 1 mL in DMSO USD 79 In-stock
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Customer Review

Based on 31 publication(s) in Google Scholar

Other Forms of Buparlisib:

Top Publications Citing Use of Products

    Buparlisib 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).

    Buparlisib 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.

    Buparlisib purchased from MCE. Usage Cited in: Prostate. 2018 Feb;78(3):166-177.

    Western blot analysis of p-AKT (Ser473) in stable cell lines (Vector-DU145 and GOLM1-DU145) treated with 200 nM, 500 nM or 1 μM BKM120.

    Buparlisib purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014.

    Representative immunoblots of control and NHARAS treated with Buparlisib for 24 h.

    Buparlisib purchased from MCE. Usage Cited in: Brain Behav. 2018 Nov;8(11):e01123.

    The effect of BKM120 on AKT phosphorylation is examined by Western blot.

    Buparlisib purchased from MCE. Usage Cited in: Cancer Lett. 2019 Jan;440-441:54-63.

    The cells are transfected with either the negative control (siNC) or BTF3 siRNA for 12 hours followed by BKM-120 or AZD-6482 treatment for 48 hours. The protein abundance is determined by an immunoblotting analysis.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Buparlisib (NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

    IC50 & Target

    p110α

    52 nM (IC50)

    p110α-H1047R

    58 nM (IC50)

    p110α-E545K

    99 nM (IC50)

    p110δ

    116 nM (IC50)

    p110β

    166 nM (IC50)

    p110γ

    262 nM (IC50)

    Vps34

    2.4 μM (IC50)

    mTOR

    4.6 μM (IC50)

    In Vitro

    Buparlisib (NVP-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]. Buparlisib (NVP-BKM120) induces multiple myeloma (MM) cell apoptosis in both dose- and time-dependent manners. Buparlisib (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 Buparlisib (NVP-BKM120) and 24-h treatment are chose in in the following experiments if not stated otherwise. Buparlisib (NVP-BKM120) treatment results in a dose-dependent growth inhibition in all tested MM cell lines. Buparlisib (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 Buparlisib (NVP-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 Buparlisib (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
    Molecular Weight

    410.39

    Formula

    C₁₈H₂₁F₃N₆O₂

    CAS No.

    944396-07-0

    SMILES

    FC(F)(C1=C(C2=CC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=NC(N)=C1)F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (243.67 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [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. Buparlisib (NVP-BKM120) supplied in DMSO (20 mM) are diluted further into DMSO (7.5 uL of 20 mM Buparlisib (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 Buparlisib (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]

    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 Buparlisib (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

    Purity: 99.90%

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    Keywords:

    BuparlisibNVP-BKM120BKM120BKM 120BKM-120PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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