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

Niraparib (Synonyms: MK-4827)

Cat. No.: HY-10619 Purity: 99.97% ee.: 99.97%
Handling Instructions

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 (MK-4827) leads to inhibition of repair of DNA damage 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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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of Niraparib:

Top Publications Citing Use of Products

    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 Oct. 

    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 Oct. 

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

    • Protocol

    • 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 (MK-4827) leads to inhibition of repair of DNA damage 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].

    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].

    Clinical Trial
    Molecular Weight

    320.39

    Formula

    C₁₉H₂₀N₄O

    CAS No.

    1038915-60-4

    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)

    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 provided by MCE.
    References
    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 Niraparib (MK-4827) is initiated. Niraparib (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 Niraparib 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.

    References

    Purity: 99.97% ee.: 99.97%

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    KeyWords:

    Niraparib | MK-4827 | MK4827 | MK 4827 | PARP | Apoptosis | poly ADP ribose polymerase | ovarian | cancer | lung | breast | DNA | damage | anti-tumor | orally | bioavailable | Inhibitor | inhibitor | inhibit

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