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VE-821ATR kinase inhibitor

VE-821

Catalog No. A2521
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $70.00 In stock
25mg $200.00 In stock
100mg $680.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

VE-821

Related Biological Data

VE-821

Related Biological Data

VE-821

Biological Activity

Description VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
Targets ATR          
IC50 13 nM/26 nM (Ki/IC50)          

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Chemical Properties

Cas No. 1232410-49-9 SDF Download SDF
Chemical Name 2-(aminomethyl)-6-[4,6-diamino-3-[4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxyoxane-3,4,5-triol;sulfuric acid
Canonical SMILES CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N
Formula C18H16N4O3S M.Wt 368.41
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Research Update

1. 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. doi: 10.4161/cbt.21093. Epub 2012 Jul 24.
Abstract
The ATR inhibitor VE-821 significantly sensitized a few pancreatic cancer cells to DNA damaging agents, radiotherapy and gemcitabine, where IT inhibited Chk1 phosphorylation and homologous recombination repair, triggered inhibition of G 2/M arrest, reduced radiosurvival and increased DNA damage in radiation- and gemcitabine-treated cancer cells.
2. 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. doi: 10.1007/s00411-013-0486-5. Epub 2013 Aug 11.
Abstract
The ATR inhibitor VE-821 exerted a more pronounced radiosenstizing effect in HL-60 cells, where it reduced phosphorylation of check-point kinase 1 and the repair of the radiation damage, inhibited G2 cell cycle arrest and induced apoptosis.

Background

VE-821 is a potent, highly-selective, and ATP-competitive DNA damage response (DDR) kinase ATR inhibitor with Ki value of 13nM. VE-821 specifically inhibits ATR, revealing low cross-reactivity against the mammalian target of rapamycin (mTOR), DNA-dependent protein kinase (DNA-PK), phosphoinositol 3-kinase-γ (PI3K) and the related PIKKs ATM [1].

HL-60 cells treated with VE-821 (10μM) showed reduction of phosphorylatin of Chk1 (Ser 345), inhibition of cell growth, and a radiosensitizing effect after Gamma-ray irradiation [2].

VE-821 has also been demonstrated to down-regulate the phosphorylated Chk1 (Ser 345) but it does not inhibit the phosphorylation of Chk2 (Thr68) and ATM (Ser1981) in pancreatic cancer cell lines, including PSN-1 and MiaPaCa-2 cells that are treated with gemcitabine or radiation. VE-821 combined with gemcitabine (a nucleoside analog) has caused a remarkable increase of cytotoxic effect of gemcitabine against hypoxia [3].

References:
[1] Reaper PM1, Griffiths MR, Long JM, Charrier JD, Maccormick S, Charlton PA, Golec JM, Pollard JR. Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR. Nat Chem Biol. 2011 Apr 13;7(7):428-30.
[2] Vávrová J1, Zárybnická L, Lukášová E, Řezáčová M, Novotná E, Sinkorová Z, Tichý A, Pejchal J, Durišová K. 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.
[3] Prevo R1, Fokas E, Reaper PM, Charlton PA, Pollard JR, McKenna WG, Muschel RJ, Brunner TB.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.