ETP-46464

Catalog No.S8050

ETP-46464 Chemical Structure

Molecular Weight(MW): 470.52

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

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USD 297 In stock
USD 970 In stock
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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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 470.52
Formula

C30H22N4O2

CAS No. 1345675-02-6
Storage powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

ATM/ATR Signaling Pathway Map

Related ATM/ATR Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID