Home PI3K/Akt/mTOR ATM/ATR inhibitor - mTOR inhibitor ETP-46464 For research use only.

ETP-46464

ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.

ETP-46464 Chemical Structure

ETP-46464 Chemical Structure

CAS No. 1345675-02-6

Purity & Quality Control

ETP-46464 Related Products

Signaling Pathway

ATM/ATR Signaling Pathways

ATM/ATR Signaling Pathway

Biological Activity

Description ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
Features Selective ATR inhibitor and particularly toxic to p53-deficient cancer cells. Often used as a pharmacologic probe due to its ideal pharmacological properties.
Targets
mTOR [1] ATR [1] DNA-PK [1] PI3Kα [1] ATM [1]
0.6 nM 14 nM 36 nM 170 nM 545 nM
In vitro
In vitro 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. [1]

Chemical Information & Solubility

Molecular Weight 470.52 Formula

C30H22N4O2
CAS No. 1345675-02-6 SDF Download ETP-46464 SDF
Smiles CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3COC2=O)C5=CC6=CC=CC=C6N=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 14 mg/mL ( (29.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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