[CAS NO. 1345675-02-6]  ETP-46464

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PRODUCTS SPECIFICATIONS [1345675-02-6]

Store
Catalog
SLK-S8050
Brand
Selleck
CAS
1345675-02-6

DESCRIPTION [1345675-02-6]

Overview

MDLMFCD23160051
Molecular Weight470.52
Molecular FormulaC30H22N4O2
SMILESN#CC(C)(C)C1=CC=C(N(C2=C3C=NC4=CC=C(C5=CC6=CC=CC=C6N=C5)C=C24)C(OC3)=O)C=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.1253 mL10.6265 mL21.2531 mL
5 mM0.4251 mL2.1253 mL4.2506 mL
10 mM0.2125 mL1.0627 mL2.1253 mL
50 mM---

Description

ETP-46464 is a potent and selective inhibitor of with 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 nM14 nM36 nM170 nM545 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.