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

pka

5.10±0.20(Predicted)

color 

Light yellow to yellow

ETP46464 Usage And Synthesis

Uses

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]

target

mTOR

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.

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