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

Niraparib tosylate hydrate (Synonyms: MK-4827 tosylate hydrate)

目录号: HY-10619E
产品使用指南

Niraparib (MK-4827) tosylate hydrate 是高效的,具有生物口服利用度的 PARP1PARP2 抑制剂,IC50 分别为 3.8 nM 和 2.1 nM。Niraparib tosylate hydrate 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 hydrate Chemical Structure

Niraparib tosylate hydrate Chemical Structure

CAS No. : 1613220-15-7

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 42 篇科研文献

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

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

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

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

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

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

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity[1][2][3].

    IC50 & Target

    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) tosylate hydrate inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. Niraparib tosylate hydrate inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. Niraparib tosylate hydrate displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay[1].
    Niraparib tosylate hydrate inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells[2].

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

    体内研究
    (In Vivo)

    Niraparib (MK-4827) tosylate hydrate is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer[1].
    Niraparib (MK-4827) tosylate hydrate is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer[1].
    Niraparib (MK-4827) tosylate hydrate is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%[1].
    Niraparib (MK-4827) tosylate hydrate enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily[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.
    分子量

    510.61

    Formula

    C26H30N4O5S

    CAS 号
    中文名称

    甲苯磺酸尼拉帕尼一水物

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    参考文献
    • 摩尔计算器

    • 稀释计算器

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    × = ×
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