Nedisertib (M3814)

For research use only.

Catalog No.S8586 Synonyms: Peposertib, MSC2490484A

Nedisertib (M3814) Chemical Structure

CAS No. 1637542-33-6

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.

Purity & Quality Control

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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

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]

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]

Protocol

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (199.2 mM)
Ethanol 2 mg/mL (4.15 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 481.91
Formula

C24H21ClFN5O3

CAS No. 1637542-33-6
Storage powder
in solvent
Synonyms Peposertib, MSC2490484A
Smiles COC1=NN=C(C=C1)C(C2=C(C=C(C(=C2)C3=NC=NC4=C3C=CC(=C4)N5CCOCC5)F)Cl)O

In vivo Formulation Calculator (Clear solution)

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04702698 Completed Drug: Peposertib Healthy Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany January 14 2021 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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DNA-PK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID