Nedisertib
Based on 31 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.70%
- CAS 番号: 1637542-33-6
- 分子式: C24H21ClFN5O3
- 分子量:481.91
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 Nedisertib
More- Nature. 2025 Aug;644(8075):241-251. [Abstract]
- Nat Methods. 2023 Sep;20(9):1388-1399. [Abstract]
- Nat Commun. 2022 Sep 8;13(1):5295. [Abstract]
- Nat Commun. 2022 Jun 27;13(1):3662. [Abstract]
- Nat Commun. 2022 Jan 25;13(1):489. [Abstract]
- Sci Immunol. 2024 Feb 2;9(92):eadi0042. [Abstract]
- Mol Cell. 2021 May 20;81(10):2216-2230.e10. [Abstract]
- Theranostics. 2023 Aug 28;13(14):4745-4761. [Abstract]
- Acta Pharm Sin B. 2021 Dec;11(12):3935-3949. [Abstract]
- Genome Biol. 2021 Aug 20;22(1):236. [Abstract]
- Cancer Immunol Res. 2025 Jun 12. [Abstract]
- Mol Cancer Ther. 2025 Jun 4;24(6):920-930. [Abstract]
- Mol Ther Nucleic Acids. 2025 Feb 1;36(1):102472. [Abstract]
- Genome Res. 2021 Mar;31(3):461-471. [Abstract]
- Int Immunopharmacol. 2026 Jun 12:185:116981. [Abstract]
- Int J Mol Sci. 2025 May 3;26(9):4361. [Abstract]
- Sci Rep. 2023 Aug 1;13(1):12429. [Abstract]
- Mol Oncol. 2023 Jul;17(7):1192-1211. [Abstract]
- Bio Protoc. 2024 Oct 20;14(20):e5085. [Abstract]
- Res Sq. 2026 Jun 17.
- bioRxiv. 2026 Jun 19.
- bioRxiv. 2026 May 13.
- bioRxiv. 2026 Jan 23:2026.01.22.701150. [Abstract]
- Patent. US20250277210A1.
- University of Wisconsin. 2025.
- Patent. US20250049807A1.
- bioRxiv. 2024 August 29.
- bioRxiv. 2024 Jul 13:2024.06.25.600671. [Abstract]
- University of British Columbia. 2024 Apr 30.
- Res Sq. 2023 Apr 6:rs.3.rs-2688694. [Abstract]
- bioRxiv. 2020 May.
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Flow Cytometry
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IF
生物活性
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DNA-PK <3 nM (IC50) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:25-300 mg/kg
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Administration:Oral administration; single dose; 10 min prior to IR
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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.
化学情報
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CAS 番号 1637542-33-6
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性状 Solid
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分子量 481.91
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分子式 C24H21ClFN5O3
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Color Light yellow to yellow
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SMILES
FC1=CC(Cl)=C([C@@H](C2=CC=C(N=N2)OC)O)C=C1C3=NC=NC4=C3C=CC(N5CCOCC5)=C4
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別名
Peposertib; M3814
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (31)
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Journal Impact Factor
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Most Recent
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Nature
2025 Aug;644(8075):241-251. PMID: 40604285 -
Nat Methods
2023 Sep;20(9):1388-1399. PMID: 37474806 -
Nat Commun
Multi-pathway DNA-repair reporters reveal competition between end-joining, single-strand annealing and homologous recombination at Cas9-induced DNA double-strand breaks. [Abstract]2022 Sep 8;13(1):5295. PMID: 36075911 -
Nat Commun
2022 Jun 27;13(1):3662. PMID: 35760797
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.
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Nat Commun
Improved gRNA secondary structures allow editing of target sites resistant to CRISPR-Cas9 cleavage. [Abstract]2022 Jan 25;13(1):489. PMID: 35078986 -
Sci Immunol
Precise CRISPR-Cas9 gene repair in autologous memory T cells to treat familial hemophagocytic lymphohistiocytosis. [Abstract]2024 Feb 2;9(92):eadi0042. PMID: 38306418 -
Mol Cell
Impact of chromatin context on Cas9-induced DNA double-strand break repair pathway balance. [Abstract]2021 May 20;81(10):2216-2230.e10. PMID: 33848455 -
Theranostics
A genome-wide CRISPR/Cas9 screen identifies DNA-PK as a sensitiser to 177Lutetium-DOTA-octreotate radionuclide therapy. [Abstract]2023 Aug 28;13(14):4745-4761. PMID: 37771787 -
Acta Pharm Sin B
2021 Dec;11(12):3935-3949. PMID: 35024317
Nedisertib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2021 Dec;11(12):3935-3949. [Abstract]
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. [Abstract]
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. [Abstract]
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. [Abstract]
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×).
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Genome Biol
Effective control of large deletions after double-strand breaks by homology-directed repair and dsODN insertion. [Abstract]2021 Aug 20;22(1):236. PMID: 34416913 -
Cancer Immunol Res
Discovery of BMS-986408, a First-In-Class Dual DGKα and DGKζ Inhibitor That Unleashes PD-1 Checkpoint and CAR T-Cell Immunotherapies. [Abstract]2025 Jun 12. PMID: 40506249 -
Mol Cancer Ther
Targeting Monounsaturated Fatty Acid Metabolism for Radiosensitization of KRAS Mutant 3D Lung Cancer Models. [Abstract]2025 Jun 4;24(6):920-930. PMID: 39834305 -
Mol Ther Nucleic Acids
Enhanced HDR-mediated correction of heterozygous COL7A1 mutations for recessive dystrophic epidermolysis bullosa. [Abstract]2025 Feb 1;36(1):102472. PMID: 40027886 -
Genome Res
2021 Mar;31(3):461-471. PMID: 33574136 -
Int Immunopharmacol
Development of super Vδ2 T cells for relapsed/refractory acute myeloid Leukemia via non-viral site-specific integration. [Abstract]2026 Jun 12:185:116981. PMID: 42284763 -
Int J Mol Sci
CRISPR/Cas9 Ribonucleoprotein Delivery Enhanced by Lipo-Xenopeptide Carriers and Homology-Directed Repair Modulators: Insights from Reporter Cell Lines. [Abstract]2025 May 3;26(9):4361. PMID: 40362595 -
Sci Rep
DNA-PK inhibition extends the therapeutic effects of Top2 poisoning to non-proliferating cells, increasing activity at a cost. [Abstract]2023 Aug 1;13(1):12429. PMID: 37528151 -
Mol Oncol
MND1 enables homologous recombination in somatic cells primarily outside the context of replication. [Abstract]2023 Jul;17(7):1192-1211. PMID: 37195379 -
Bio Protoc
Expansion and Precise CRISPR-Cas9 Gene Repair of Autologous T-Memory Stem Cells from Patients with T-Cell Immunodeficiencies. [Abstract]2024 Oct 20;14(20):e5085. PMID: 39512884 -
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bioRxiv
2026 Jan 23:2026.01.22.701150. PMID: 41648153 -
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bioRxiv
Scalable intracellular delivery via microfluidic vortex shedding enhances the function of chimeric antigen receptor T-cells. [Abstract]2024 Jul 13:2024.06.25.600671. PMID: 38979201 -
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Res Sq
Haploinsufficiency of ZNF251 causes DNA-PKcs-dependent resistance to PARP inhibitors in BRCA1-mutated cancer cells. [Abstract]2023 Apr 6:rs.3.rs-2688694. PMID: 37066268 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (282 KB)
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SDS (393 KB)
- 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)
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取扱説明書 (2659 KB)
参考文献
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 |