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  • 5 mg - 85 EUR
  • 25 mg - 199 EUR
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datasheet

VE-821

VE-821 was described as a potent and selective inhibitor of protein kinase ATR. The compound acts as an ATP competitor with IC50 value of 50 nM for ATR at 50 microM ATP. It exhibited no significant activity against a panel of 50 kinases. A synthetic lethal interaction between ATR and the ATM-p53 pathway was shown in cells treated with DNA-damaging agents. VE-821 significantly enhanced the sensitivity of pancreatic cancer cells to radiation. ATR inhibition by VE-821 led to suppression of radiation-induced G2/M arrest in cancer cells and reduced cancer cell survival, accompanied by increased DNA damage and inhibition of homologous recombination repair. Growth arrest induced by ATR inhibition in normal cells is reversible and VE-821 does not induce cytotoxicity in normal cells.

catalogue number: V134
synonyms: -
CAS: 1232410-49-9
MW: 368.41 g/mol

References
Cancer Biol Ther. 2012 Sep;13(11):1072-81. PMID: 22825331
Br J Cancer. 2012 Jul 10;107(2):291-9. PMID: 22713662
Nat Chem Biol. 2011 Apr 13;7(7):428-30. PMID: 21490603
7th NCRI Cancer Conference, 6-9 November 2011, Liverpool, UK Meeting abstract LB64