Nedisertib

• Description:

  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 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, protect from light, stored under nitrogen)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• CAS Number:

  1637542-33-6