ETP-46464

Catalog No.S8050

For research use only.

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

ETP-46464 Chemical Structure

CAS No. 1345675-02-6

Selleck's ETP-46464 has been cited by 4 Publications

Purity & Quality Control

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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

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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 6 mg/mL
(12.75 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 470.52
Formula

C30H22N4O2

CAS No. 1345675-02-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3COC2=O)C5=CC6=CC=CC=C6N=C5

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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