ETP46464

Synonym(s):2-Methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile;4-[4-(1-Isocyano-1-methyl-ethyl)-phenyl]-6-quinolin-3-yl-1,4-dihydro-2-oxa-4,9-diaza-phenanthren-3-one;ATRi

CAS NO.：1345675-02-6
Empirical Formula: C30H22N4O2
Molecular Weight: 470.52
MDL number: MFCD23160051
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-19 23:02:33

What is ETP46464?

The Uses of ETP46464

ETP-46464 is used as an ATR inhibitor in the treatment of cancer-associated mutations.

Biological Activity

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]

References

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.

Properties of ETP46464

Boiling point:	709.3±60.0 °C(Predicted)
Density	1.310±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	≥16.13 mg/mL in DMSO
form	solid
pka	5.10±0.20(Predicted)
color	Light yellow to yellow