An ATR inhibitor (IC50 = 25 nM) that also inhibits mTOR and DNA-PK (IC50s = 0.6 and 36 nM

ETP-46464 – 5 mg

Brand:
Cayman
CAS:
1345675-02-6
Storage:
-20
UN-No:
Non-Hazardous - /

ETP-46464 is an inhibitor of the DNA damage response kinase Ataxia-telangiectasia mutated (ATM)- and Rad3-related (ATR) with an IC50 value of 25 nM.{31719} It also inhibits mTOR and DNA-dependent protein kinase (IC50s = 0.6 and 36 nM, respectively), and is moderately active against PI3Kα and ATM (IC50s = 170 and 545 nM, respectively).{31719} Pharmacological inhibition of ATR is reported to generate replicative stress, leading to chromosomal breakage in the presence of conditions that stall replication forks.{31719} ETP-46464 has been shown to be toxic to p53-deficient cells, which is exacerbated by replicative stress-generating conditions such as the overexpression of cyclin E.{31719}  

 

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Description

An ATR inhibitor (IC50 = 25 nM) that also inhibits mTOR and DNA-PK (IC50s = 0.6 and 36 nM, respectively); generates replicative stress, leading to chromosomal breakage in the presence of conditions that stall replication forks

Formal name: α,α-dimethyl-4-[2-oxo-9-(3-quinolinyl)-2H-[1,3]oxazino[5,4-c]quinolin-1(4H)-yl]-benzeneacetonitrile

Synonyms:  ATM Inhibitor III|ATR Inhibitor III

Molecular weight: 470.5

CAS: 1345675-02-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|ATM||Product Type|Biochemicals|Kinase Inhibitors|DNA-PK||Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling||Research Area|Cancer|DNA Damage and Repair||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Epigenetics, Transcription, & Translation|RNA, DNA, & Protein Synthesis

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