925701-46-8

Basic information

• Product Name: KU 60019
• Synonyms: (2R,6S)-rel-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide;2-((2R,6S)-2,6-Dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl
• CAS NO: 925701-46-8
• Molecular Formula: C₃₀H₃₃N₃O₅S
• Molecular Weight: 547.68
• Mol File: 925701-46-8.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 786.6±60.0 °C(Predicted)
• Appearance: /
• Density: 1.314±0.06 g/cm3 (20 ºC 760 Torr)
• PKA: 13.52±0.20(Predicted)
• CAS DataBase Reference: KU 60019(CAS DataBase Reference)
• NIST Chemistry Reference: KU 60019(925701-46-8)
• EPA Substance Registry System: KU 60019(925701-46-8)

Safety Data

• Hazardous Substances Data: 925701-46-8(Hazardous Substances Data)

Usage

Description

KU 60019 is a potent and reversible inhibitor of Ataxia-telangiectasia mutated (ATM) kinase, a serine/threonine kinase that plays a crucial role in activating checkpoint signaling following double strand DNA breaks and genotoxic stress. With an IC50 of 6.3 nM, KU 60019 effectively blocks the phosphorylation of ATM substrate proteins and is much less effective or without effect against a panel of 229 other kinases.

Uses

Used in Cancer Therapy:
KU 60019 is used as a radiosensitizer for glioma cells, enhancing their sensitivity to radiation and improving treatment outcomes. It is particularly effective in producing lethality in cells with mutant p53 or those deficient in PTEN, making it a promising candidate for targeted cancer therapy.
Used in In Vitro Cancer Research:
KU 60019 is used as an inhibitor to study the role of ATM kinase in the migration and invasion of glioma cells in vitro. This helps researchers understand the underlying mechanisms of cancer progression and identify potential therapeutic targets.
Used in Orthotopic Xenograft Models:
KU 60019 is used in orthotopic xenograft models of glioblastoma multiforme to evaluate its radiosensitization effects and increase survival rates when administered intra-tumoral. This application aids in assessing the drug's potential in clinical settings and its impact on tumor growth and progression.

Upstream product

• 587871-49-6 2-(7-amino-9H-thioxanthen-4-yl)-6-morpholin-4-yl-pyran-4-one 
• 79-04-9 chloroacetyl chloride 

Relevant articles and documents

ATM INHIBITOR

A compound of formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, and their use in treating diseases ameliorated by the inhibition of ATM.