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

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

Cat. No.: HY-10619E Purity: 99.97%
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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

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5 mg USD 70 In-stock
10 mg USD 100 In-stock
50 mg USD 180 In-stock
100 mg USD 280 In-stock
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Based on 55 publication(s) in Google Scholar

Other Forms of Niraparib tosylate hydrate:

Niraparib tosylate hydrate Related Antibodies

Top Publications Citing Use of Products

52 Publications Citing Use of MCE Niraparib tosylate hydrate

Proliferation Assay
WB

    Niraparib tosylate hydrate purchased from MedChemExpress. 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 tosylate hydrate purchased from MedChemExpress. 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 tosylate hydrate purchased from MedChemExpress. 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.

    View All PARP Isoform Specific Products:

    View All Isoforms
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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    • Purity & Documentation

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    • 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].

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

    Niraparib tosylate hydrate Related Antibodies
    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].

    MedChemExpress (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

    510.61

    Formula

    C26H30N4O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC(C1=CC=CC2=CN(C3=CC=C([C@H]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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (97.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9584 mL 9.7922 mL 19.5844 mL
    5 mM 0.3917 mL 1.9584 mL 3.9169 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9584 mL 9.7922 mL 19.5844 mL 48.9610 mL
    5 mM 0.3917 mL 1.9584 mL 3.9169 mL 9.7922 mL
    10 mM 0.1958 mL 0.9792 mL 1.9584 mL 4.8961 mL
    15 mM 0.1306 mL 0.6528 mL 1.3056 mL 3.2641 mL
    20 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4481 mL
    25 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9584 mL
    30 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6320 mL
    40 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2240 mL
    50 mM 0.0392 mL 0.1958 mL 0.3917 mL 0.9792 mL
    60 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8160 mL
    80 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 mL
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    Niraparib tosylate hydrate Related Classifications

    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.

    Keywords:

    Niraparib tosylate1613220-15-7MK-4827 tosylatePARPApoptosispoly ADP ribose polymerase ovariancancerlungbreastDNAdamageanti-tumororallybioavailableInhibitorinhibitorinhibit

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