Nedisertib

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].

Product Specifications

CAS Number

[1637542-33-6]

Product Name Alternative

Peposertib; M3814

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

BCRP; DNA-PK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Membrane Transporter/Ion Channel; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/M3814.html

Concentration

10mM

Purity

99.70

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C24H21ClFN5O3

Molecular Weight

481.91

Precautions

H302, H315, H319, H335

References & Citations

[1]L. Damstrup, et al. M3814, a DNA-dependent Protein Kinase Inhibitor (DNA-PKi), Potentiates the Effect of Ionizing Radiation (IR) in Xenotransplanted Tumors in Nude Mice. IJROBP. 2016; 94, 940-941.|[2]Thomas Fuchss, et al. Arylchinazoline. WO2014183850A1. 2014-11-20.|[3]Wu ZX, et al. M3814, a DNA-PK Inhibitor, Modulates ABCG2-Mediated Multidrug Resistance in Lung Cancer Cells. Front Oncol. 2020 May 12;10:674.