1337531-36-8

1337531-36-8 structure

Name: GSK2606414
Chemical Name: 1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone
CAS Number: 1337531-36-8
Molecular Formula: C₂₄H₂₀F₃N₅O
Molecular Weight: 451.444
Catalog: Biochemical Inhibitor Apoptosis PERK inhibitor
Create Date: 2017-12-11 18:43:44
Modify Date: 2024-01-04 19:35:39
GSK2606414 is a cell-permeable and orally available PERK inhibitor with an IC50 of 0.4 nM.

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

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.

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

3680-69-1

1337531-36-8

Literature: Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. Journal of Medicinal Chemistry, 2012 , vol. 55, # 16 p. 7193 - 7207