ETP-46464
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 470.52 |
| Cas No. | 1345675-02-6 |
| Formula | C30H22N4O2 |
| Solubility | ≥16.13 mg/mL in DMSO |
| Chemical Name | 2-methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile |
| SDF | Download SDF |
| 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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 & MSDS
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Chemical structure
