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

Buparlisib  (Synonyms: 布帕尼西; BKM120; NVP-BKM120)

目录号: HY-70063 纯度: 99.82%
COA 产品使用指南

摩尔计算器

Buparlisib (BKM120; NVP-BKM120) 是一种 pan-class I PI3K 抑制剂，作用于 p110α/p110β/p110δ/p110γ，IC50 分别为 52 nM/166 nM/116 nM/262 nM。

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Buparlisib Chemical Structure

Buparlisib Chemical Structure

CAS No. : 944396-07-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥715
In-stock
5 mg ￥650
In-stock
10 mg ￥920
In-stock
50 mg ￥1850
In-stock
100 mg ￥2780
In-stock
200 mg ￥4200
In-stock
500 mg 现货 询价
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Buparlisib:

Buparlisib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 68 篇科研文献

WB

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

    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.

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

    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.  [Abstract]

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

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

    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: Nat Med. 2016 Jul;22(7):723-6.  [Abstract]

    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: Oncogene. 2016 Jul 7;35(27):3607-12.  [Abstract]

    (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).

    查看 PI3K 亚型特异性产品:

    查看所有亚型
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Buparlisib (BKM120; 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[1]

    p110α

    52 nM (IC50)

    p110β

    166 nM (IC50)

    p110δ

    116 nM (IC50)

    p110γ

    262 nM (IC50)

    Vps34

    2.4 μM (IC50)

    p110α-H1047R

    58 nM (IC50)

    p110α-E545K

    99 nM (IC50)

    mTOR

    4.6 μM (IC50)

    体外研究
    (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Buparlisib 相关抗体:
    体内研究
    (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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    410.39

    Formula

    C18H21F3N6O2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    布帕尼西
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (243.67 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.09 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 50% PEG300    50% Saline

      Solubility: 2.08 mg/mL (5.07 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    COA (288 KB) HNMR (192 KB) LCMS (122 KB)

    产品使用指南 (1538 KB)
    参考文献
    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.
    参考文献

    Buparlisib 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4367 mL 12.1835 mL 24.3671 mL 60.9177 mL
    5 mM 0.4873 mL 2.4367 mL 4.8734 mL 12.1835 mL
    10 mM 0.2437 mL 1.2184 mL 2.4367 mL 6.0918 mL
    15 mM 0.1624 mL 0.8122 mL 1.6245 mL 4.0612 mL
    20 mM 0.1218 mL 0.6092 mL 1.2184 mL 3.0459 mL
    25 mM 0.0975 mL 0.4873 mL 0.9747 mL 2.4367 mL
    30 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0306 mL
    40 mM 0.0609 mL 0.3046 mL 0.6092 mL 1.5229 mL
    50 mM 0.0487 mL 0.2437 mL 0.4873 mL 1.2184 mL
    60 mM 0.0406 mL 0.2031 mL 0.4061 mL 1.0153 mL
    80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7615 mL
    100 mM 0.0244 mL 0.1218 mL 0.2437 mL 0.6092 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Buparlisib944396-07-0BKM120 NVP-BKM120布帕尼西BKM 120BKM-120PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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