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

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

Cat. No.: HY-10619E
Handling Instructions

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.

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

Niraparib tosylate hydrate Chemical Structure

Niraparib tosylate hydrate Chemical Structure

CAS No. : 1613220-15-7

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other In-stock Forms of Niraparib tosylate hydrate:

Other Forms of Niraparib tosylate hydrate:

Top Publications Citing Use of Products

42 Publications Citing Use of MCE Niraparib tosylate hydrate

    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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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)

    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.

    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.
    Molecular Weight

    510.61

    Formula

    C26H30N4O5S

    CAS No.
    SMILES

    NC(C1=CC=CC2=CN(C3=CC=C([[email protected]]4CNCCC4)C=C3)N=C21)=O.O=S(C5=CC=C(C)C=C5)(O)=O.O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

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

    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Niraparib tosylate hydrate
    Cat. No.:
    HY-10619E
    Quantity:
    MCE Japan Authorized Agent: