2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. PARP Apoptosis
  4. Niraparib tosylate

Niraparib tosylate  (Synonyms: 尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate)

目录号: HY-10619B 纯度: 99.99%
COA 产品使用指南

摩尔计算器

Niraparib tosylate (MK-4827 tosylate) 是一种高效的，具有生物口服利用度的 PARP1 和 PARP2 抑制剂，IC50 分别为 3.8 和 2.1 nM。Niraparib tosylate 抑制 DNA 损伤修复，诱导凋亡 (apoptosis) 并具有抗肿瘤活性。

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Niraparib tosylate Chemical Structure

Niraparib tosylate Chemical Structure

CAS No. : 1038915-73-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥672
In-stock
1 mg ￥310
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2 mg ￥498
In-stock
5 mg ￥620
In-stock
10 mg ￥1050
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50 mg ￥4100
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100 mg ￥5900
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Niraparib tosylate:

Niraparib tosylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 57 篇科研文献

Proliferation Assay
WB

    Niraparib tosylate purchased from MCE. Usage Cited in: Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568.  [Abstract]

    CDK4 is evaluated via western blot analysis in different cell lines with the treatment of Niraparib in different concentrations and times.

    Niraparib tosylate purchased from MCE. Usage Cited in: Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568.  [Abstract]

    Cyclin D is evaluated via western blot analysis in different cell lines with the treatment of Niraparib in different concentrations and times.

    Niraparib tosylate purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867.  [Abstract]

    PARP1 inhibition is lethal to MPM cells. Colony formation assays of clonal cell survival with continuous Niraparib or AZD2281.

    查看 PARP 亚型特异性产品:

    查看所有亚型
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

    IC50 & Target[1]

    PARP-2

    2.1 nM (IC50)

    PARP-1

    3.8 nM (IC50)

    V-PARP

    330 nM (IC50)

    TANK-1

    570 nM (IC50)

    PARP-3

    1300 nM (IC50)

    体外研究
    (In Vitro)

    Niraparib (MK-4827) 在全细胞试验中抑制 PARP 活性，EC50=4 nM 和 EC90=45 nM。MK-4827 抑制突变体 BRCA-1 和 BRCA-2 癌细胞的增殖，CC50 在 10-100 nM 范围内。MK-4827 在全细胞试验中表现出出色的 PARP 1 和 2 抑制作用，IC50 分别为 3.8 和 2.1 nM[1]。
    为了验证 Niraparib (MK-4827) 在这些细胞系中抑制 PARP，A549 和 H1299 细胞用 1 μM Niraparib (MK-4827) 处理不同时间，并使用化学发光测定法测量 PARP 酶活性。结果表明，Niraparib (MK-4827) 在处理后 15 分钟内抑制 PARP，A549 细胞在 1 小时达到约 85% 的抑制，H1299 细胞在 1 小时达到约 55% 的抑制[2]。

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

    Niraparib tosylate 相关抗体:
    体内研究
    (In Vivo)

    Niraparib (MK-4827) 具有良好的耐受性，并在 BRCA-1 缺陷癌症的异种移植模型中显示出作为单一药物的疗效。Niraparib (MK-4827) 在体内具有良好的耐受性，并且在 BRCA-1 缺陷癌症的异种移植模型中显示出作为单一药物的疗效。Niraparib (MK-4827) 在大鼠中的药代动力学可接受，血浆清除率为 28 (mL/min)/kg，分布容积非常高 (Vdss=6.9 L/kg)，长末端半衰期 (t1/2=3.4 h)，生物利用度极佳，F=65%[1]。
    Niraparib (MK-4827) 在两种情况下均增强 p53 突变体 Calu-6 肿瘤的放射反应，单次每日剂量 50 mg/kg 比每日两次 25 mg/kg 更有效[3]。

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

    492.59

    Formula

    C26H28N4O4S
    CAS 号
    性状

    固体

    颜色

    White to yellow

    中文名称

    尼拉帕尼对苯甲磺酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (203.01 mM; 超声助溶 (<60°C); 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 : 1 mg/mL (2.03 mM; heat to 50°C)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0301 mL 10.1504 mL 20.3009 mL
    5 mM 0.4060 mL 2.0301 mL 4.0602 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, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.08 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.08 mM); 澄清溶液

    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）。

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    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: 99.99%

    COA (201 KB) HNMR (282 KB) LCMS (94 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    The inhibition of PARP is analyzed in A549 and H1299 cells using the HT Universal Chemiluminescent PARP Assay Kit. Briefly, cells are treated with DMSO or 1 μM Niraparib (MK-4827) for 15, 30, 60, or 120 minutes, trypsinized, and transferred to a pre-chilled tube. The cells are washed twice with ice cold PBS and resuspended in cold PARP extraction buffer. The cell suspensions are incubated on ice for 30 minutes with periodic vortexing to disrupt the cell membrane. The suspensions are centrifuged and the supernatant transferred to a pre-chilled tube on ice. The histone coated wells of the 96-well plate are rehydrated with 1X PARP buffer and incubated at room temperature for 30 minutes. The PARP buffer is removed and 20 μg of protein as determined by the Bio-Rad Protein Assay is added to each well followed by diluted PARP-HSA enzyme and 1X PARP buffer. The strip wells are then incubated at room temperature for 60 minutes, washed twice with PBS containing 0.1% Triton X-100, and then washed with PBS. Diluted Strep-HRP is added to the strip wells and incubated for 60 minutes at room temperature. The wells are washed again as before. Equal volumes of PeroxyGlow A and B are combined and added to the wells and chemiluminescent readings are obtained immediately using a plate-reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Female nude mice (Ncr Nu/Nu) are randomly assigned to treatment groups consisting of 5 to 8 mice each when tumors grew to 6.0 mm in diameter at which time treatment with MK-4827 is initiated. MK-4827 is given at a dose of 25 mg/kg twice daily or 50 mg/kg once daily for either 21 days or is discontinued at 9 days from the time tumors reached 8 mm in diameter. Fractionated local tumor irradiation (XRT) is given when tumors reach 8.0 mm in diameter (7.7-8.2 mm). Radiation (2 Gy per fraction) is delivered to the tumor-bearing leg of mice once daily for 14 consecutive days or twice daily for 7 consecutive days using a small-animal irradiator consisting of two parallel-opposed 137Cs sources, at a dose rate of 5 Gy/min. During irradiation un-anesthetized mice are mechanically immobilized in a jig so that the tumor is centered within a 3.0 cm diameter radiation field and the animal’s body shielded from radiation exposure. On the day when both MK-4827 and radiation are given, drug is administered 1 h before the first radiation dose of the day.

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

    Niraparib tosylate 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, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.0301 mL 10.1504 mL 20.3009 mL 50.7521 mL
    DMSO 5 mM 0.4060 mL 2.0301 mL 4.0602 mL 10.1504 mL
    10 mM 0.2030 mL 1.0150 mL 2.0301 mL 5.0752 mL
    15 mM 0.1353 mL 0.6767 mL 1.3534 mL 3.3835 mL
    20 mM 0.1015 mL 0.5075 mL 1.0150 mL 2.5376 mL
    25 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0301 mL
    30 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
    40 mM 0.0508 mL 0.2538 mL 0.5075 mL 1.2688 mL
    50 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0150 mL
    60 mM 0.0338 mL 0.1692 mL 0.3383 mL 0.8459 mL
    80 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6344 mL
    100 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5075 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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:

    Niraparib1038915-73-9MK-4827尼拉帕尼对苯甲磺酸盐MK4827MK 4827PARPApoptosispoly ADP ribose polymerase ovariancancerlungbreastDNAdamageanti-tumororallybioavailableInhibitorinhibitorinhibit

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