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

Niraparib  (Synonyms: 尼拉帕尼; MK-4827)

目錄號: HY-10619 純度: 99.96%
COA 產(chǎn)品使用指南

Niraparib (MK-4827) 是高效的,具有生物口服利用度的 PARP1PARP2 抑制劑,IC50 分別為 3.8 nM 和 2.1 nM。Niraparib 抑制 DNA 損傷修復(fù),誘導(dǎo)凋亡 (apoptosis) 并具有抗腫瘤活性。

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Niraparib Chemical Structure

Niraparib Chemical Structure

CAS No. : 1038915-60-4

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10 mM * 1 mL in DMSO ¥682
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Customer Review

Other Forms of Niraparib:

MCE 顧客使用本產(chǎn)品發(fā)表的 59 篇科研文獻(xiàn)

Proliferation Assay
WB

    Niraparib 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 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 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.
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib 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)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 IC50
    4 nM
    Compound: 8, MK-4827
    Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
    Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
    [PMID: 25761096]
    A549 CC50
    11 nM
    Compound: 8, MK-4827
    Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    [PMID: 25761096]
    A549 CC50
    1760 nM
    Compound: 8, MK-4827
    Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    [PMID: 25761096]
    BT-20 CC50
    2200 nM
    Compound: 8, MK-4827
    Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    [PMID: 25761096]
    CAPAN-1 IC50
    3.5 nM
    Compound: 8, MK-4827
    Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
    Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
    [PMID: 25761096]
    CAPAN-1 CC50
    90 nM
    Compound: 56, MK-4827
    Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay
    Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay
    [PMID: 19873981]
    DLD-1 IC50
    0.149 μM
    Compound: 3
    Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
    Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days
    [PMID: 34570508]
    DoTc2-4510 CC50
    23 nM
    Compound: 8, MK-4827
    Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    [PMID: 25761096]
    HeLa CC50
    33 nM
    Compound: 56, MK-4827
    Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay
    Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay
    [PMID: 19873981]
    HeLa CC50
    34 nM
    Compound: 8, MK-4827
    Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay
    Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay
    [PMID: 25761096]
    HeLa EC50
    4 nM
    Compound: 8, MK-4827
    Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
    Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
    [PMID: 25761096]
    HeLa CC50
    852 nM
    Compound: 8, MK-4827
    Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    [PMID: 25761096]
    HeLa CC50
    860 nM
    Compound: 56, MK-4827
    Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay
    Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay
    [PMID: 19873981]
    HMEC CC50
    > 5000 nM
    Compound: 56, MK-4827
    Antiproliferative activity against HMEC after 6 to 7 days by cell titer-blue assay
    Antiproliferative activity against HMEC after 6 to 7 days by cell titer-blue assay
    [PMID: 19873981]
    HT-22 IC50
    35 μM
    Compound: 50
    Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
    Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
    [PMID: 36876904]
    Jurkat EC50
    0.2 μM
    Compound: MK-4827
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide
    [PMID: 23850199]
    Jurkat EC50
    31 μM
    Compound: MK-4827
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay
    Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay
    [PMID: 23850199]
    MDA-MB-231 IC50
    33.22 μM
    Compound: Niraparib
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
    [PMID: 36512711]
    MDA-MB-231 IC50
    60.91 μM
    Compound: Niraparib
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of nutlin-3 by CCK-8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of nutlin-3 by CCK-8 assay
    [PMID: 36512711]
    MDA-MB-436 CC50
    18 nM
    Compound: 56, MK-4827
    Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay
    Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay
    [PMID: 19873981]
    MDA-MB-468 IC50
    7.6 μM
    Compound: Niraparib
    Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay
    Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay
    [PMID: 33200929]
    PrEC CC50
    > 5000 nM
    Compound: 56, MK-4827
    Antiproliferative activity against human PrEC cells after 6 to 7 days by cell titer-blue assay
    Antiproliferative activity against human PrEC cells after 6 to 7 days by cell titer-blue assay
    [PMID: 19873981]
    SUM149PT CC50
    24 nM
    Compound: 8, MK-4827
    Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay
    [PMID: 25761096]
    體外研究
    (In Vitro)

    Niraparib (MK-4827) 在全細(xì)胞測定中抑制 PARP 活性,EC50=4 nM,EC90=45 nM。Niraparib 抑制突變型 BRCA-1 和 BRCA-2 癌細(xì)胞的增殖,CC50 在 10-100 nM 范圍內(nèi)。Niraparib 在全細(xì)胞測定中分別表現(xiàn)出優(yōu)異的 PARP 1 和 2 抑制效果[1]。為了驗(yàn)證 Niraparib (MK-4827) 在這些細(xì)胞系中抑制 PARP,用 1 μM Niraparib 處理 A549 和 H1299 細(xì)胞不同時(shí)間,并使用化學(xué)發(fā)光測定法測量 PARP 酶活性。結(jié)果表明,Niraparib 在治療后 15 分鐘內(nèi)抑制 PARP,在 A549 細(xì)胞中 1 小時(shí)的抑制率達(dá)到約 85%,在 H1299 細(xì)胞中 1 小時(shí)的抑制率達(dá)到約 55%[2]。

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

    體內(nèi)研究
    (In Vivo)

    Niraparib 在體內(nèi)耐受性良好,在 BRCA-1 缺陷癌癥異種移植模型中作為單一藥物表現(xiàn)出療效。Niraparib (MK-4827) 的特點(diǎn)是大鼠的藥代動力學(xué)可接受,血漿清除率為 28 (mL/min)/kg,分布容積極高 (Vdss=6.9 L/kg),終末半衰期長 (t1/2=3.4 h),生物利用度極高,F(xiàn)=65%[1]。Niraparib 在兩種情況下均增強(qiáng)了 p53 突變型 Calu-6 腫瘤的放射反應(yīng),單日劑量 50 mg/kg 比每日兩次 25 mg/kg 更有效[3]。

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

    Animal Model: Female nude mice (Ncr Nu/Nu) with solitary tumor xenografts[3]
    Dosage: 25 mg/kg or 50 mg/kg
    Administration: Gavage, 25 mg/kg twice a day with 6 h between doses or 50 mg/kg once daily for 21 consecutive days
    Result: Enhanced radiation response.
    Clinical Trial
    分子量

    320.39

    Formula

    C19H20N4O

    CAS 號
    性狀

    固體

    顏色

    White to light yellow

    中文名稱

    尼拉帕尼

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 31.25 mg/mL (97.54 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

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

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.1212 mL 15.6060 mL 31.2120 mL
    5 mM 0.6242 mL 3.1212 mL 6.2424 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗(yàn):

    請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.49 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.49 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.96%

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1212 mL 15.6060 mL 31.2120 mL 78.0299 mL
    5 mM 0.6242 mL 3.1212 mL 6.2424 mL 15.6060 mL
    10 mM 0.3121 mL 1.5606 mL 3.1212 mL 7.8030 mL
    15 mM 0.2081 mL 1.0404 mL 2.0808 mL 5.2020 mL
    20 mM 0.1561 mL 0.7803 mL 1.5606 mL 3.9015 mL
    25 mM 0.1248 mL 0.6242 mL 1.2485 mL 3.1212 mL
    30 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6010 mL
    40 mM 0.0780 mL 0.3901 mL 0.7803 mL 1.9507 mL
    50 mM 0.0624 mL 0.3121 mL 0.6242 mL 1.5606 mL
    60 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3005 mL
    80 mM 0.0390 mL 0.1951 mL 0.3901 mL 0.9754 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.

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    產(chǎn)品名稱:
    Niraparib
    目錄號:
    HY-10619
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