[CAS NO. 1337531-36-8] GSK2606414

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PRODUCTS SPECIFICATIONS [1337531-36-8]

Catalog

SLK-S7307

Brand

Selleck

CAS

1337531-36-8

DESCRIPTION [1337531-36-8]

Overview

MDL	MFCD25976926
Molecular Weight	451.44
Molecular Formula	C24H20F3N5O
SMILES	NC1=C2C(=CN(C)C2=NC=N1)C=3C=C4C(=CC3)N(C(CC5=CC(C(F)(F)F)=CC=C5)=O)CC4

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

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2151 mL	11.0757 mL	22.1513 mL
5 mM	0.4430 mL	2.2151 mL	4.4303 mL
10 mM	0.2215 mL	1.1076 mL	2.2151 mL
50 mM	0.0443 mL	0.2215 mL	0.4430 mL

Description

GSK2606414 is an orally available, potent, and selective inhibitor with of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced in NB cells with MYCN amplification. GSK2606414 exacerbates in HCT116 cells while reduces the in SIL1 KD HeLa cells.

Features

The first PERK-selective inhibitor with good oral bioavailability and crosses the blood-brain barrier.

Targets

EIF2AK3 (PERK) ^[1]
(Cell-free assay)

0.4 nM

In vitro

GSK2606414 inhibits PERK Autophosphorylation in A459 Cells with IC50 of <0.3 μM.

References

[1] Axten JM, et al. J Med Chem. 2012, 55(16), 7193-7207.

Synonyms

Ethanone, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-(trifluoromethyl)phenyl]-

1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone

7-Methyl-5-[1-[[3-(trifluoromethyl)phenyl]acetyl]-2,3-dihydro-1H-indol-5-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

GSK 2606414

1-[5-(4-Amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone