GSK 2606414

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Cat.No. 5107 - GSK 2606414 | C24H20F3N5O | CAS No. 1337531-36-8
Description: Potent and selective PERK inhibitor; orally bioavailable
Chemical Name: 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
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. Inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancreatic human tumor xenograft growth in mice. Orally bioavailable.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

Compound Libraries

GSK 2606414 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 451.44
Formula C24H20F3N5O
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1337531-36-8
PubChem ID 53469448
InChI Key SIXVRXARNAVBTC-UHFFFAOYSA-N
Smiles NC1=NC=NC2=C1C(C3=CC(CCN4C(CC5=CC=CC(C(F)(F)F)=C5)=O)=C4C=C3)=CN2C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.14 100

Preparing Stock Solutions

The following data is based on the product molecular weight 451.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.22 mL 11.08 mL 22.15 mL
5 mM 0.44 mL 2.22 mL 4.43 mL
10 mM 0.22 mL 1.11 mL 2.22 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Axten et al (2012) Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J.Med.Chem. 55 7193 PMID: 22827572

Harding et al (2012) Uncoupling proteostasis and development in vitro with a small molecule inhibitor of the pancreatic endoplasmic reticulum kinase, PERK. J.Biol.Chem. 287 44338 PMID: 23148209


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Keywords: GSK2606414 potent selective protein kinase R-like ER kinase PERK orally bioavailable antitumor ER-stress PERK

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