VE-821

VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.

Product Specifications

CAS Number

[1232410-49-9]

UNSPSC

12352005

Hazard Statement

H302

Target

ATM/ATR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/VE-821.html

Purity

99.67

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1=CC=CC=C1)C2=NC(C3=CC=C(C=C3)S(=O)(C)=O)=CN=C2N

Molecular Formula

C18H16N4O3S

Molecular Weight

368.41

Precautions

H302

References & Citations

[1]Reaper PM, 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.|[2]Charrier JD, et al. Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents. J Med Chem. 2011 Apr 14;54 (7) :2320-30.|[3]Prevo R, 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.|[4]Muralidharan SV, et al. BET bromodomain inhibitors synergize with ATR inhibitors to induce DNA damage, apoptosis, senescence-associated secretory pathway and ER stress in Myc-induced lymphoma cells. Oncogene. 2016 Sep 8;35 (36) :4689-97.