VE-821
VE-821 is an inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase, a chromatin-remodeling protein that senses DNA damage and activates the DNA damage checkpoint to induce cell cycle arrest. VE-821 exhibits anticancer activity, inducing chromosome fragmentation, apoptosis, and cell death in vitro. VE-821 decreases phosphorylation of Chk1 and induces G2 phase cell cycle arrest in pancreatic cancer cells and leukemia cells, sensitizing them to the effects of radiation.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18978766
| Cas No. |
1232410-49-9 |
|---|---|
| Purity |
≥98% |
| Formula |
C18H16N4O3S |
| Formula Wt. |
368.41 |
| IUPAC Name |
3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide |
| Synonym |
VE821 |
| Appearance |
Light yellow powder |
Flynn RL, Cox KE, Jeitany M, et al. Alternative lengthening of telomeres renders cancer cells hypersensitive to ATR inhibitors. Science. 2015 Jan 16;347(6219):273-7. PMID: 25593184.
Vávrová J, Zárybnická L, Lukášová E, et al. Inhibition of ATR kinase with the selective inhibitor VE-821 results in radiosensitization of cells of promyelocytic leukaemia (HL-60). Radiat Environ Biophys. 2013 Nov;52(4):471-9. PMID: 23934411.
Prevo R, Fokas E, Reaper PM, et al. The novel ATR inhibitor VE-821 increases sensitivity of pancreatic cancer cells to radiation and chemotherapy. Cancer Biol Ther. 2012 Sep;13(11):1072-81. PMID: 22825331.
Reaper PM, Griffiths MR, Long JM, et al. Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR. Nat Chem Biol. 2011 Apr 13;7(7):428-30. PMID: 21490603.
