Home DNA Damage/DNA Repair DNA-PK inhibitor Nedisertib (M3814) For research use only.

Nedisertib (M3814)

Synonyms: Peposertib, MSC2490484A

Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.

Nedisertib (M3814) Chemical Structure

Nedisertib (M3814) Chemical Structure

CAS No. 1637542-33-6

Purity & Quality Control

Products often used together with Nedisertib (M3814)

L755507

Nedisertib and L755507 significantly contribute to precise gene editing for single-base modifications in Stargardt disease patients.

Siles L, et al. Mol Ther Nucleic Acids. 2023 Mar 3;32:64-79.

L755507

Nedisertib and L755507 significantly contribute to precise gene editing for single-base modifications in Stargardt disease patients.

Siles L, et al. Mol Ther Nucleic Acids. 2023 Mar 3;32:64-79.

Nedisertib (M3814) Related Products

Signaling Pathway

DNA-PK Signaling Pathways

DNA-PK Signaling Pathway

Biological Activity

Description Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.
Targets
DNA-PK [1]
(Cell-free assay)
3 nM
In vitro
In vitro

M3814 potently inhibits DNA-PK catalytic activity and sensitizes multiple cancer cell lines to ionizing radiation (IR) and DSB-inducing agents. Inhibition of DNA-PK autophosphorylation in cancer cells leads to an increased number of persistent DSBs.[2]
Cell Research Cell lines 92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs)
Concentrations 5 μmol/L–5 nmol/L
Incubation Time 120 h
Method

Radiosensitization of 92 cancer cell lines and resting peripheral blood mononuclear cells (PBMCs) by M3814 is performed at Oncolead. Cell viability is determined with 3 Gy IR, M3814 (5 μmol/L–5 nmol/L), and a combination of 3 Gy IR and M3814 (5 μmol/L–5 nmol/L). Treated cells are incubated for 120 hours, fixed, stained with sulforhodamine B, and quantified colorimetrically.
In Vivo
In vivo

Inhibition of DNA-PK autophosphorylation in xenograft tumors leads to an increased number of persistent DSBs. Oral administration of M3814 to two xenograft models of human cancer, using a clinically established 6-week fractionated radiation schedule, strongly potentiates the antitumor activity of IR and lead to complete tumor regression at nontoxic doses.[2]
Animal Research Animal Models 7- to 9-week-old female NMRI (nu/nu) mice
Dosages 5 mg/kg, 25 mg/kg, 100 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04702698 Completed
Healthy
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 January 14 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 481.91 Formula

C24H21ClFN5O3
CAS No. 1637542-33-6 SDF --
Smiles COC1=NN=C(C=C1)C(C2=C(C=C(C(=C2)C3=NC=NC4=C3C=CC(=C4)N5CCOCC5)F)Cl)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (199.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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