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GSK2606414

Names

[ CAS No. ]:
1337531-36-8

[ Name ]:
GSK2606414

[Synonym ]:
CS-1428
QC-9698
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
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]-
7-methyl-5-(1-([3-(trifluoromethyl)phenyl]acetyl)-2,3-dihydro-1H-indol-5-yI)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
S7307
GSK2606414
GSK-2606414

Biological Activity

[Description]:

GSK2606414 is a cell-permeable and orally available PERK inhibitor with an IC50 of 0.4 nM.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PERK
Research Areas >> Cancer

[Target]

EIF2AK3 (PERK):0.4 nM (IC50)

EIF2AK1 (HRI):420 nM (IC50)

EIF2AK2 (PKR):696 nM (IC50)


[In Vitro]

GSK2606414 inhibits PERK activation in cells[1]. 

[In Vivo]

GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice[1].

[Animal admin]

Exponentially growing BxPC3 tumor cells (10×106 cells/mouse) from cell culture are implanted subcutaneously into the right flank of female nude mice. Sixteen days after implantation, mice with -200 mm3 tumors are randomized into various treatment groups (n=8 mice/group). Animals are orally treated with vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water, pH 4.8), compound at 50 or 150 mg/kg, b.i.d. for 21 days. Tumor volume is measured twice weekly with calipers and calculated. Results are represented as percent inhibition on completion of dosing, which is 100[1-(average growth of drug-treated population)/(average growth of vehicle-treated control population)]. Statistical analysis is performed using a two-tailed t test.

[References]

[1]. Axten JM, et al. 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 reticulu

[2]. Zhang M, et al. Inhibiting the Plasmodium eIF2α Kinase PK4 Prevents Artemisinin-Induced Latency. Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4.


[Related Small Molecules]

GSK2656157 | ISRIB | CCT020312

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
720.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H20F3N5O

[ Molecular Weight ]:
451.444

[ Flash Point ]:
389.4±32.9 °C

[ Exact Mass ]:
451.161987

[ PSA ]:
77.04000

[ LogP ]:
4.53

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.668

[ Storage condition ]:
-20°C

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream