product name ETP-46464
Description: ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. 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.
References: Nat Struct Mol Biol. 2011 Jun;18(6):721-7.
470.52
Formula
C30H22N4O2
CAS No.
1345675-02-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 6 mg/mL (12.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19395336
| In Vitro |
Kinase Assay: Cell Assay: ETP-46464 shows almost full activity against ATR at 100 nM. ETP-46464 inhibits the activity of PI3Kα, mTOR and DNA-PKcs with IC50s of 170, 0.6 and 36 nM. ETP-46464 is able to promote the breakage of stalled replication forks. Exposure to ETP-46464 leads the generation of substantial amounts of DNA damage in replicating cells. 1 μM ETP-46464 abrogates the ionizing radiation-induced G2/M checkpoint and leads to the presence of micronuclei or completely fragmented nuclei in cells. ETP-46464 is particularly toxic for p53-deficient cells, which is exacerbated by replicative stress-generating conditions such as the overexpression of cyclin E. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nat Struct Mol Biol. 2011 Jun;18(6):721-7. |
Related Posts
product name ETP-46464
Description: ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. 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.
References: Nat Struct Mol Biol. 2011 Jun;18(6):721-7.
470.52
Formula
C30H22N4O2
CAS No.
1345675-02-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 6 mg/mL (12.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19395336
| In Vitro |
Kinase Assay: Cell Assay: ETP-46464 shows almost full activity against ATR at 100 nM. ETP-46464 inhibits the activity of PI3Kα, mTOR and DNA-PKcs with IC50s of 170, 0.6 and 36 nM. ETP-46464 is able to promote the breakage of stalled replication forks. Exposure to ETP-46464 leads the generation of substantial amounts of DNA damage in replicating cells. 1 μM ETP-46464 abrogates the ionizing radiation-induced G2/M checkpoint and leads to the presence of micronuclei or completely fragmented nuclei in cells. ETP-46464 is particularly toxic for p53-deficient cells, which is exacerbated by replicative stress-generating conditions such as the overexpression of cyclin E. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nat Struct Mol Biol. 2011 Jun;18(6):721-7. |