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

Niraparib (Synonyms: MK-4827)

Cat. No.: HY-10619 Purity: 99.96%
Handling Instructions

Niraparib (MK-4827) est un inhibiteur très puissant et biodisponible oralement de PARP1 et de PARP2 avec des IC50s de 3,8 et 2,1 nM, respectivement. Niraparib entraîne l'inhibition de la réparation des dommages à l'ADN, active l'apoptose et montre une activité anti-tumorale.

Niraparib (MK-4827) ist ein hochpotenter und oral bioverfügbarer PARP1 und PARP2-Inhibitor mit IC50-Werten von 3,8 bzw. 2,1 nM. Niraparib führt zur Hemmung der Reparatur von DNA-Schäden, aktiviert die apoptosis und zeigt Anti-Tumor-Aktivität..

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.

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

Niraparib Chemical Structure

Niraparib Chemical Structure

CAS No. : 1038915-60-4

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Estimated Time of Arrival: December 31
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10 mg USD 100 In-stock
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50 mg USD 180 In-stock
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100 mg USD 280 In-stock
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Customer Review

Based on 46 publication(s) in Google Scholar

Other Forms of Niraparib:

Top Publications Citing Use of Products

43 Publications Citing Use of MCE Niraparib

    Niraparib 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 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 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    In Vitro

    Niraparib (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay[1]. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) 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.

    In Vivo

    Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) 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) 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.
    Clinical Trial
    Molecular Weight

    320.39

    Formula

    C19H20N4O

    CAS No.
    SMILES

    NC(C1=CC=CC2=CN(C3=CC=C([[email protected]]4CNCCC4)C=C3)N=C21)=O

    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 : 25 mg/mL (78.03 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.3121 mL 1.5606 mL 3.1212 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: ≥ 2.08 mg/mL (6.49 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.96%

    References
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    Product Name:
    Niraparib
    Cat. No.:
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