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Nedisertib {[allProObj[0].p_purity_real_show]}

货号：A778486 同义名： M3814; Peposertib

Nedisertib是一个口服可用的DNA依赖性蛋白激酶（DNA-PK）抑制剂，具有潜在的抗肿瘤和化疗/放疗增敏作用。

Nedisertib 化学结构 CAS号：1637542-33-6
Nedisertib 化学结构
CAS号：1637542-33-6
Nedisertib 3D分子结构
CAS号：1637542-33-6
Nedisertib 化学结构 CAS号：1637542-33-6
Nedisertib 3D分子结构 CAS号：1637542-33-6
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Nedisertib 纯度/质量文件 产品仅供科研

货号：A778486 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 DNA-PK ↓ 其他靶点 纯度
PI-103 ++

DNA-PK, IC50: 23 nM

 		99%+
CC-115 +++

DNA-PK, IC50: 0.013 μM

 		mTOR 98+%
Samotolisib ✔ 99%+
NU 7026 +

DNA-PK, IC50: 0.23 μM

 		PI3K 98+%
PIK-75 HCl ++++

DNA-PK, IC50: 2 nM

 		99%+
PP121 +

DNA-PK, IC50: 60 nM

 		VEGFR,PDGFR 99%+
KU-0060648 ++++

DNA-PK, IC50: 5 nM

 		98%
KU-57788 +++

DNA-PK, IC50: 14 nM

 		99%+
LTURM34 ++

DNA-PK, IC50: 0.034 μM

 		98%+
SF2523 +++

DNA-PK, IC50: 9 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Nedisertib 生物活性

描述 M-3814, also known as MSC2490484A and nedisertib, is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, the DNA-PK inhibitor MSC2490484A binds to and inhibits the activity of DNA-PK. This inhibits the ability of tumor cells to repair damaged DNA, which may lead to a reduction in cellular proliferation of cancer cells expressing DNA-PK.

Nedisertib 细胞实验

Cell Line
Concentration Treated Time Description References
HeLa cells 1 mM 1 hour To study the binding mode of Nedisertib with DNA-PKcs and reveal its molecular mechanism as a selective DNA-PKcs inhibitor Nature. 2022 Jan;601(7894):643-648.
SKNBE-2 cells 1 µM 14 days To evaluate the effect of Nedisertib in combination with LuTate on the sensitivity of SKNBE-2 cells. Results showed that the combination of 20 MBq/mL LuTate and 1 μM Nedisertib reduced cell survival to less than 20%. Theranostics. 2023 Aug 28;13(14):4745-4761.
AR42J cells 0.5 µM or 1 µM 14 days To evaluate the effect of Nedisertib in combination with LuTate on the sensitivity of AR42J cells. Results showed that Nedisertib enhanced the cytotoxic effect of LuTate, but the effect was less pronounced than in H1299-7 cells. Theranostics. 2023 Aug 28;13(14):4745-4761.
H1299-7 cells 0.5 µM or 1 µM 14 days To evaluate the effect of Nedisertib in combination with LuTate on the sensitivity of H1299-7 cells. Results showed that Nedisertib significantly enhanced the cytotoxic effect of LuTate, especially when combined with 10 MBq/mL LuTate and 1 μM Nedisertib, reducing cell survival to less than 0.01%. Theranostics. 2023 Aug 28;13(14):4745-4761.
NCI-H460 1 µM 17 days To evaluate the cytotoxic effect of peposertib on NCI-H460 cells, results showed that 1 μM peposertib alone had no discernable effect on clonogenic survival, but when combined with IR (2 Gy), there was a significant loss of clonogenic survival. Cancer Res. 2022 Oct 17;82(20):3815-3829.
A549 1 µM 17 days To evaluate the cytotoxic effect of peposertib on A549 cells, results showed that 1 μM peposertib alone had no discernable effect on clonogenic survival, but when combined with IR (2 Gy), there was a significant loss of clonogenic survival. Cancer Res. 2022 Oct 17;82(20):3815-3829.
KPC2 1 µM 25 hours To evaluate the radiosensitizing effect of M3814 on KPC2 cells, results showed that M3814 significantly enhanced radiation-induced cell death. Mol Cancer Res. 2022 Jul 6;20(7):1137-1150.
Panc1 1 µM 25 hours To evaluate the radiosensitizing effect of M3814 on Panc1 cells, results showed that M3814 significantly enhanced radiation-induced cell death. Mol Cancer Res. 2022 Jul 6;20(7):1137-1150.
CT26 cells 10 µM 30 minutes To evaluate the effect of M3814 on the radiosensitivity of CT26 cells, results showed that M3814 significantly reduced cell viability and increased the proportion of γH2AX-positive cells indicating DNA damage. Neoplasia. 2022 Mar;25:53-61.
SW837 cells 10 µM 30 minutes To evaluate the effect of M3814 on the radiosensitivity of SW837 cells, results showed that M3814 significantly reduced cell viability and increased the proportion of γH2AX-positive cells indicating DNA damage. Neoplasia. 2022 Mar;25:53-61.
UPCI-SCC-154 300 nM 30 minutes Assessed the effect of DNA-PKcs inhibition on cell cycle distribution, showing significant G2/M accumulation in HPV+ cells Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
UM-SCC-104 300 nM 30 minutes Assessed the effect of DNA-PKcs inhibition on cell cycle distribution, showing significant G2/M accumulation in HPV+ cells Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
UD-SCC-2 300 nM 30 minutes Assessed the effect of DNA-PKcs inhibition on cell cycle distribution, showing significant G2/M accumulation in HPV+ cells Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
UM-SCC-14A 300 nM 30 minutes Assessed the effect of DNA-PKcs inhibition on cell cycle distribution, showing significant G2/M accumulation in p53-mutated cells Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
UM-SCC-10B 300 nM 30 minutes Assessed the effect of DNA-PKcs inhibition on cell cycle distribution, showing significant G2/M accumulation in p53-mutated cells Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
UM-SCC-74A 300 nM 30 minutes Assessed the effect of DNA-PKcs inhibition on cell cycle distribution, showing no substantial G2/M accumulation in p53 WT cells Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
UM-SCC-17B 300 nM 30 minutes Assessed the effect of DNA-PKcs inhibition on cell cycle distribution, showing no substantial G2/M accumulation in p53 WT cells Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
THP-1 1 µM 4 hours To evaluate the effect of M3814 on IR-induced p53 target gene expression. Results showed that M3814 did not enhance p53 target gene expression in p53-deficient cells. Sci Rep. 2021 Jun 9;11(1):12148.
MV4-11 1 µM 4 hours To evaluate the effect of M3814 on IR-induced p53 target gene expression. Results showed that M3814 enhanced the expression of p53 target genes. Sci Rep. 2021 Jun 9;11(1):12148.
MOLM-13 1 µM 4 hours To evaluate the effect of M3814 on IR-induced p53 apoptotic signaling. Results showed that M3814 enhanced the ATM/p53 signaling pathway, leading to increased p53 protein levels and transcriptional activity. Sci Rep. 2021 Jun 9;11(1):12148.
697 cells 0.5 µM, 1 µM, 1.5 µM 48 hours To study the effect of Nedisertib on V(D)J recombination, results showed significant reduction in coding joint formation at 1 μM and 1.5 μM concentrations Mol Immunol. 2020 Apr;120:93-100.
U2OS 5 µM 5 days To evaluate the effect of peposertib on MMEJ reporter activity, results showed that peposertib treatment increased MMEJ reporter activity. Cancer Res. 2022 Oct 17;82(20):3815-3829.
LMS05 400 nM 6 days To evaluate the effect of peposertib on LMS cell viability, results showed that peposertib significantly reduced the viability of LMS cells. Clin Cancer Res. 2023 Dec 15;29(24):5128-5139.
LMS04 400 nM 6 days To evaluate the effect of peposertib on LMS cell viability, results showed that peposertib significantly reduced the viability of LMS cells. Clin Cancer Res. 2023 Dec 15;29(24):5128-5139.
LMS03 400 nM 6 days To evaluate the effect of peposertib on LMS cell viability, results showed that peposertib significantly reduced the viability of LMS cells. Clin Cancer Res. 2023 Dec 15;29(24):5128-5139.
HEK293/ABCG2-WT 1 µM 72 hours M3814 can significantly reverse ABCG2-mediated multidrug resistance, increasing the intracellular accumulation of ABCG2 substrate drugs such as mitoxantrone and doxorubicin. Front Oncol. 2020 May 12;10:674.
A549/MX10 1 µM 72 hours M3814 can significantly reverse ABCG2-mediated multidrug resistance, increasing the intracellular accumulation of ABCG2 substrate drugs such as mitoxantrone and doxorubicin. Front Oncol. 2020 May 12;10:674.
NCI-H460/MX20 1 µM 72 hours M3814 can significantly reverse ABCG2-mediated multidrug resistance, increasing the intracellular accumulation of ABCG2 substrate drugs such as mitoxantrone and doxorubicin. Front Oncol. 2020 May 12;10:674.
SKNBE-2 cells 1 μM 4 hours Evaluate the cytotoxic effect of LuTate on SKNBE-2 cells, showing significant reduction in cell survival at 10 MBq/mL and 20 MBq/mL concentrations, with enhanced effect when combined with DNA-PK inhibitor nedisertib. Theranostics. 2023 Aug 28;13(14):4745-4761.
AR42J cells 0.5 μM or 1 μM 4 hours Evaluate the cytotoxic effect of LuTate on AR42J cells, showing significant reduction in cell survival at 5 MBq/mL and 10 MBq/mL concentrations, with enhanced effect when combined with DNA-PK inhibitor nedisertib. Theranostics. 2023 Aug 28;13(14):4745-4761.

Nedisertib 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
NRG mice TP53 mutant ovarian tumors (DF59 PDX model) Oral 100 mg/kg Once daily for 4 weeks To evaluate the in vivo antitumor effect of combined peposertib and NVB treatment on TP53 mutant ovarian tumors, results showed that NVB monotherapy significantly inhibited tumor growth, while peposertib monotherapy had no significant effect, but the combination therapy further enhanced tumor growth inhibition. Cancer Res. 2022 Oct 17;82(20):3815-3829.
NMRI-nu mice Subcutaneous xenograft model Oral 100 mg/kg Five consecutive days Evaluated the effect of DNA-PKcs inhibition combined with radiotherapy on tumor growth, showing more durable responses in HPV+ UD-SCC-2 xenografts Mol Cancer Ther. 2025 Feb 4;24(2):214-229.
BALB/c nude mice H1299-7 and AR42J xenograft models Oral 150 mg/kg Once daily for 6 consecutive days To evaluate the effect of Nedisertib in combination with LuTate on tumor growth and survival. Results showed that the combination therapy significantly inhibited tumor growth and prolonged survival. In the H1299-7 model, the combination extended median survival to 30 days; in the AR42J model, the combination extended median survival to 35 days. Theranostics. 2023 Aug 28;13(14):4745-4761.
C57BL/6 mice MT4 pancreatic cancer model Oral 25 mg/kg Administered 1 hour before radiation on day 0, followed by administration alone on days 1-4 To evaluate the antitumor efficacy of M3814 combined with radiation in the mT4 pancreatic cancer model, results showed that the combination therapy significantly inhibited tumor growth. Mol Cancer Res. 2022 Jul 6;20(7):1137-1150.
NRG mice AML patient-derived xenograft model Oral gavage 25 mg/kg Twice daily for 14 days To evaluate the efficacy of M3814 in combination with CPX-351 for AML treatment. Results showed that the combination treatment significantly reduced AML cell burden without increasing hematopoietic toxicity. Sci Rep. 2021 Jun 9;11(1):12148.
BALB/c mice CT26 subcutaneous tumor model Oral gavage 50 mg/kg 5 days per week for 2 weeks To evaluate the effect of M3814 in combination with standard treatment on the CT26 subcutaneous tumor model, results showed that M3814 significantly increased the clinical complete response rate but did not significantly affect the pathological complete response rate. Neoplasia. 2022 Mar;25:53-61.
Mice LMS04 xenograft and LMSPDX1 PDX models Peposertib oral, doxorubicin intravenous peposertib 100 mg/kg BID, doxorubicin 0.5–1 mg/kg qw Peposertib twice daily, doxorubicin once weekly, until tumor volume exceeded 2000 mm3 To evaluate the efficacy of combination therapy with peposertib and low-dose doxorubicin in LMS mouse models, results showed that the combination therapy significantly inhibited tumor growth. Clin Cancer Res. 2023 Dec 15;29(24):5128-5139.

Nedisertib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02316197 Advanced Solid Tumors ... 展开 >> Chronic Lymphocytic Leukemia 收起 << Phase 1 Completed - Germany ... 展开 >> Please contact the Merck KGaA Communication Center Darmstadt, Germany 收起 <<
NCT02516813 Advanced Solid Tumors Phase 1 Recruiting January 8, 2021 United States, California ... 展开 >> Research site Recruiting Fresno, California, United States, 93720 United States, Florida Research site Recruiting Fort Lauderdale, Florida, United States, 33308 Research site Recruiting Miami, Florida, United States, 33136-1002 United States, Montana Research site Recruiting Billings, Montana, United States, 59101 United States, New York Research site Recruiting Bronx, New York, United States, 10461 United States, Pennsylvania Research site Recruiting Philadelphia, Pennsylvania, United States, 19107 United States, Texas Research site Not yet recruiting Houston, Texas, United States, 77030 United States, Washington Research site Completed Tacoma, Washington, United States, 98405 Belgium Research site Active, not recruiting Leuven, Belgium Denmark Research site Recruiting Copenhagen, Denmark, 2100 Research site Recruiting Herlev, Denmark Germany Research site Active, not recruiting Freiburg, Baden Wuerttemberg, Germany, 79106 Research site Recruiting Heidelberg, Baden Wuerttemberg, Germany Research site Recruiting Mannheim, Baden Wuerttemberg, Germany Research site Recruiting Tuebingen, Baden Wuerttemberg, Germany, 72076 Research site Recruiting Mainz, Rhineland-Palatinate, Germany, 55131 Research site Recruiting Dresden, Sachsen, Germany, 1307 Research site Recruiting Kiel, Schleswig-Holstein, Germany, 24105 Research site Recruiting Berlin, Germany, 12200 Netherlands Research site Recruiting Amsterdam, Netherlands, 1066 CX Research site 1 Active, not recruiting Amsterdam, Netherlands Norway Research site Active, not recruiting Oslo, Norway Sweden Research site Recruiting Solna, Sweden, 17176 收起 <<
NCT03724890 Oncology Soli... 展开 >>d Tumors 收起 << Phase 1 Recruiting October 9, 2020 United States, Florida ... 展开 >> H. Lee Moffitt Cancer Center and Research Institute, Inc Recruiting Tampa, Florida, United States, 33612 United States, Tennessee Tennessee Oncology- DDU Recruiting Nashville, Tennessee, United States, 37205 收起 <<

Nedisertib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.38mL

2.08mL

1.04mL

20.75mL

4.15mL

2.08mL

Nedisertib 技术信息

CAS号1637542-33-6
分子式C24H21ClFN5O3
分子量 481.91
SMILES Code O[C@@H](C1=CC(C2=C3C=CC(N4CCOCC4)=CC3=NC=N2)=C(F)C=C1Cl)C5=NN=C(OC)C=C5
MDL No. MFCD31619234
别名 M3814; Peposertib; MSC2490484A
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

Tags: Nedisertib | M3814;Peposertib;MSC2490484A | DNA-PK | AmBeed-信号通路专用抑制剂 | Nedisertib 纯度/质量文件 | Nedisertib 亚型比较 | Nedisertib 生物活性 | Nedisertib 临床数据 | Nedisertib 实验方案 | Nedisertib 技术信息

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