ETP46464

ETP46464 Basic information
Product Name:ETP46464
Synonyms:Benzeneacetonitrile, α,α-dimethyl-4-[2-oxo-9-(3-quinolinyl)-2H-[1,3]oxazino[5,4-c]quinolin-1(4H)-yl]-;alpha,alpha-Dimethyl-4-[2-oxo-9-(3-quinolinyl)-2H-[1,3]oxazino[5,4-c]quinolin-1(4H)-yl]-benzeneacetonitrile ETP46464;2-methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile;ETP46464;alpha,alpha-Dimethyl-4-[2-oxo-9-(3-quinolinyl)-2H-[1,3]oxazino[5,4-c]quinolin-1(4H)-yl]-benzeneacetonitrile;ETP 46464; ETP46464;2-Methyl-2-(4-(2-oxo-9-(quinolin-3-yl)-2,4-dihydro-1H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl);ETP46464 USP/EP/BP
CAS:1345675-02-6
MF:C30H22N4O2
MW:470.52
EINECS:
Product Categories:Inhibitors;PI3K/Akt/mTOR;Akt;mTOR;PI3K
Mol File:1345675-02-6.mol
ETP46464 Structure
ETP46464 Chemical Properties
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
pka5.10±0.20(Predicted)
Safety Information
MSDS Information
ETP46464 Usage And Synthesis
UsesETP-46464 is used as an ATR inhibitor in the treatment of cancer-associated mutations.
Biological Activityetp-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]
targetmTOR
references1. 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.
ETP46464 Preparation Products And Raw materials
PHA-680632 VE 822 ABT 737 ABT-199 Selumetinib KU-55933 (ATM Kinase Inhibitor)

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