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ETP-46464ATR inhibitor,potent and selective

ETP-46464

Catalog No. A8626
Size Price Stock 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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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

ETP-46464

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  

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Chemical Properties

Cas No. 1345675-02-6 SDF Download SDF
Chemical Name 2-methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile
Canonical SMILES CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3COC2=O)C5=CC6=CC=CC=C6N=C5
Formula C30H22N4O2 M.Wt 470.52
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips N/A
Shipping Condition N/A

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.