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ETP-46464

In stock
Catalog No.
A8626
ATR inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$100.00
In stock
5mg
$90.00
In stock
10mg
$150.00
In stock
25mg
$350.00
In stock
50mg
$630.00
In stock

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Email: [email protected]

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Background

ETP-46464 is a potent and selective inhibitor for ATR (IC50 = 25 nM).

ATR (ATM- and Rad3-related) is a member of PIKK (phosphatidylinositol 3-kinase-like kinases) that regulates the DNA damage response pathways. It is a DNA damage sensor that is activated upon genotoxic stresses (e.g. ionizing radiation, UV radiation and DNA replication stalling) and phosphorylates its downstream substrates (e.g. p53, BRCA1 and CHEK1).

ETP-46464 abolished the G2/M checkpoint. It caused the presence of micronuclei or completely fragmented nuclei in cells under ionizing radiation. Cells treated simultaneously with hydroxyurea and ETP-46464 exhibited elevated ATM and Chk2 phosphorylation. In U2OS cells, ETP-46464 promoted the breakage of stalked replication forks. [1]

Reference:
1. Toledo LI, Murga M, Zur R et al.  A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. Nat Struct Mol Biol. 2011 Jun;18(6):721-7.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt470.52
Cas No.1345675-02-6
FormulaC30H22N4O2
Solubility≥16.13mg/mL in DMSO
Chemical Name2-methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile
SDFDownload SDF
Canonical SMILESCC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3COC2=O)C5=CC6=CC=CC=C6N=C5
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Biological Activity

Description ETP-46464 is a potent and selective inhibitor of ATR with an IC50 value of 25 nM.
Targets mTOR ATR DNA-PK PI3Kα ATM  
IC50 0.6 nM 14 nM 36 nM 170 nM 545 nM  

Quality Control

Chemical structure

ETP-46464