Chemical Name |
VE-821 |
CAS Number |
1232410-49-9 |
MDL Number |
MFCD19443686 |
Molecular Formula |
C18H16N4O3S |
Molecular Weight |
368.41 |
Introduction of 1232410-49-9 :
VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM. IC50 & Target: Ki: 13 nM (ATR)[1]
IC50: 26 nM (ATR)[2] In Vitro: VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3Kγ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases[1]. VE-821 (compound 27) also inhibits ATM and DNA-PK wirh IC50 of >8 μM, and 4.4 μM, respectively[2]. VE-821 significantly enhances the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and Gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 leads to inhibition of radiation-induced G2/M arrest in cancer cells. In both PSN-1 and MiaPaCa-2 cells, 1 µM VE-821 inhibits phosphorylation of Chk1 (Ser 345) after treatment with Gemcitabine (100 nM), radiation (6 Gy) or both, at 2 h post-irradiation[3].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.