2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Membrane Transporter/Ion Channel
  3. DNA-PK BCRP
  4. Nedisertib

Nedisertib  (Synonyms: Peposertib; M3814)

Cat. No.: HY-101570 Purity: 99.70%
COA
SDS
Handling Instructions Technical Support

Nedisertib (M3814) est un inhibiteur de DNA-PK qui est puissant sélectif disponible par voie orale , avec un IC50 de <3 nM. Activité anti-tumorale.

Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity.

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

CAS No. : 1637542-33-6

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Nedisertib:

Nedisertib Related Antibodies

Top Publications Citing Use of Products

    Nedisertib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jun 27;13(1):3662.  [Abstract]

    Effect of DNAPKcs kinase inhibitor M3814 (3 days) on No Indel EJ in HEK293 cells with XLF-WT, XLF-K160D, and without XLF was examined.

    Nedisertib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Dec;11(12):3935-3949.

    Cell viability curves of NSCLC cell lines A549 treated with paclitaxel (PTX) and etoposide (Etop), in the absence or presence of M3814 (5 mmol/L) for 48 h were analyzed.

    Nedisertib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Dec;11(12):3935-3949.

    Quantitative data of the EdU-positive fraction. Representative images of colonies from colony formation assays in A549, H460, and H1703 cells treated with paclitaxel (5 nmol/L) and etoposide (100 nmol/L) in the absence or presence of M3814 (5 μmol/L) for 18 h, followed by incubation in 6-well plates for another 14 days.

    Nedisertib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Dec;11(12):3935-3949.

    NSCLC cell lines A549, H460, and H1703 were treated with paclitaxel (5 nmol/L) and etoposide (100 nmol/L) with or without M3814 (5 mmol/L) for 48 h, stained with Annexin V/PI, and evaluated through flow cytometry.

    Nedisertib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Dec;11(12):3935-3949.

    Representative images of NSCLC cells incubated in the presence or absence of 5 mmol/L M3814 for 1 h before adding 100 nmol/L paclitaxel or 1 mmol/L etoposide. Following extensive washing in drug-free medium, cells were incubated with or without 5 mmol/L M3814 for another 4 h, and immunostained for γ-H2AX (red) foci. DAPI staining (blue fluorescence), scale bar = 10 μm (magnification, 1000×).

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity[1][2][3].

    IC50 & Target[3]

    DNA-PK

    <3 nM (IC50)

    In Vitro

    Nedisertib (0.3-1 µM; 72 h) significantly enhances the cytotoxicity of ABCG2 substrate drugs Mitoxantrone (HY-13502) and Doxorubicin (HY-15142A) in ABCG2-overexpressing lung cancer cell lines NCI-H460/MX20 and A549/MX10, reversing multidrug resistance[1].

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

    Nedisertib Related Antibodies
    In Vivo

    Nedisertib (25-300 mg/kg; oral administration; single dose) enhances the antitumor effect of ionizing radiation in multiple xenograft tumor models[2].

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

    Animal Model: 6 human xenograft models (HCT116, FaDu, NCI-H460, A549, Capan-1, BxPC3) in mice representing 4 different cancer types (colon, head and neck, lung, and pancreas) treated ionizing radiation (IR)[2]
    Dosage: 25-300 mg/kg
    Administration: Oral administration; single dose; 10 min prior to IR
    Result: Significantly inhibited tumor growth in all 6 models in combination with IR.
    Induced tumor regression in FaDu and NCI-H460 models, and showed no tumor regrowth in the FaDu model with the combination of 25 and 50 mg/kg and IR (total 60 Gy).
    Had no significant weight loss or visual signs of toxicity in mice.
    Molecular Weight

    481.91

    Formula

    C24H21ClFN5O3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    FC1=CC(Cl)=C([C@@H](C2=CC=C(N=N2)OC)O)C=C1C3=NC=NC4=C3C=CC(N5CCOCC5)=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (103.75 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 2.0751 mL 10.3754 mL 20.7508 mL
    5 mM 0.4150 mL 2.0751 mL 4.1502 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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:  1% CMC-Na/5% Tween-80 in Saline water

      Solubility: 5.56 mg/mL (11.54 mM); Suspended solution; Need ultrasonic

    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (5.19 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.
    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 (protect from light, stored under nitrogen)

    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

    Purity: 99.70%

    SDS (393 KB)

    COA (259 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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 (protect from light, stored under nitrogen). 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 2.0751 mL 10.3754 mL 20.7508 mL 51.8769 mL
    5 mM 0.4150 mL 2.0751 mL 4.1502 mL 10.3754 mL
    10 mM 0.2075 mL 1.0375 mL 2.0751 mL 5.1877 mL
    15 mM 0.1383 mL 0.6917 mL 1.3834 mL 3.4585 mL
    20 mM 0.1038 mL 0.5188 mL 1.0375 mL 2.5938 mL
    25 mM 0.0830 mL 0.4150 mL 0.8300 mL 2.0751 mL
    30 mM 0.0692 mL 0.3458 mL 0.6917 mL 1.7292 mL
    40 mM 0.0519 mL 0.2594 mL 0.5188 mL 1.2969 mL
    50 mM 0.0415 mL 0.2075 mL 0.4150 mL 1.0375 mL
    60 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8646 mL
    80 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6485 mL
    100 mM 0.0208 mL 0.1038 mL 0.2075 mL 0.5188 mL
    • 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.

    Nedisertib 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:

    Nedisertib1637542-33-6Peposertib M3814M3814M 3814M-3814DNA-PKBCRPDNA-dependent protein kinaseBreast cancer resistance proteinABCG2HCT116FaDuNCI-H460A549Capan-1BxPC3Inhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Nedisertib
    Cat. No.:
    HY-101570
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.