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VE-821

(CAS No:1232410-49-9)
VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
CAS No:1232410-49-9
Molecular Weight(MW):368.41
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 1232410-49-9
Molecular formula(MF) C18H16N4O3S
Molecular Weight(MW): 368.41
Alias
Solubility
In vitro DMSO 74 mg/mL (200.86 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
Biological Activity
Description VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
Targets
ATR [1]
(Cell-free assay)
13 nM(Ki)
In vitro

VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3K (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively. VE-821 alone commits a large fraction of cancer cell populations to death, but it only reversibly limits cell cycle progression in normal cells, with minimal death or long-term detrimental effects. VE-821 along with cisplatin treatment shows the most marked synergy. [1] VE-821 inhibits H2AX cell growth with IC50 of 800 nM. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U2OS  Growth Inhibition Assay IC50～0.8 μM 25593184
SAOS2 Growth Inhibition Assay IC50～0.8 μM 25593184
CAL72 Growth Inhibition Assay IC50～0.8 μM 25593184
NOS1 Growth Inhibition Assay IC50～0.8 μM 25593184
HUO9 Growth Inhibition Assay IC50～0.8 μM 25593184
MG63 Growth Inhibition Assay IC50～9 μM 25593184
SJSA1 Growth Inhibition Assay IC50～9 μM 25593184
MDA-MB-231 Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
HT-29 Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
HCT-116 p53+/+ Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
HCT-116 p53-/- Cytotoxicity Assay 1/3/10 μM 1 h potentiates the cytotoxicity of both camptothecin and LMP-400 25269479
TF-1 Growth Inhibition Assay 0.011–8 μM 96 h enhances the antiproliferative effects of MK1775 24179152
HEL Growth Inhibition Assay 0.011–8 μM 96 h enhances the antiproliferative effects of MK1775 24179152
THP-1 Growth Inhibition Assay 0.011–8 μM 96 h enhances the antiproliferative effects of MK1775 24179152
HL-60  Function Assay 10 mM 0.5 h reduces phosphorylation of Chk1 at serine 345 23934411
OVCAR-8  Function Assay 1 µM  24 h abrogates chemotherapy-induced cell cycle arrest 23548269
PANC-1 Growth Inhibition Assay 0.11-9 μM 1 h inhibits the cell viability in a dose- dependent manner 22825331
MiaPaCa Growth Inhibition Assay 0.11-9 μM 1 h inhibits the cell viability in a dose- dependent manner 22825331
PSN-1 Growth Inhibition Assay 0.11-9 μM 1 h inhibits the cell viability in a dose- dependent manner 22825331

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