Ku-60019 – 5 mg

Brand:
Cayman
CAS:
925701-46-8
Storage:
-20
UN-No:
Non-Hazardous - /

Ataxia-telangiectasia mutated (ATM) is a serine/threonine kinase that activates checkpoint signaling following double strand DNA breaks and genotoxic stress. Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins.{28729,28730} It is much less effective or without effect against a panel of 229 other kinases.{28729} Ku-60019 sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro.{28729,28730} It produces radiosensitization and increases survival in vivo when administered intra-tumorally in orthotopic xenograft models of glioblastoma multiforme.{28728} Ku-60019 is particularly effective in producing lethality in cells with mutant p53 or that are deficient in PTEN.{28728,28731}  

 

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Description

A potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins; sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro; produces radiosensitization and increases survival in vivo when administered intra-tumorally


Formal name: rel-2R,6S-dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide

Synonyms: 

Molecular weight: 547.7

CAS: 925701-46-8

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|ATM||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|ATM Signaling