- VE-821
- AZ20
- KU 55933
- KU-60019
- CGK733
| ETP-46464ATR inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.57%
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Chemical structure
| 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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| 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 | ≥16.13mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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.
