GSK2606414

Modify Date: 2024-01-04 19:35:39

GSK2606414 Structure
GSK2606414 structure
 Common Name GSK2606414
CAS Number 1337531-36-8 Molecular Weight 451.444
Density 1.4±0.1 g/cm3 Boiling Point 720.3±60.0 °C at 760 mmHg
Molecular Formula C24H20F3N5O Melting Point N/A
MSDS N/A Flash Point 389.4±32.9 °C

 Use of GSK2606414


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

 Names

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

 GSK2606414 Biological Activity

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

 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

4-Chloro-7H-pyrrolo[2,3-d]pyrimidine structure

4-Chloro-7H-pyr...

CAS#:3680-69-1

~%

GSK2606414 Structure

GSK2606414

CAS#: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
5-Bromoindoline structure

5-Bromoindoline

CAS#:22190-33-6

~%

GSK2606414 Structure

GSK2606414

CAS#: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
tert-butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate structure

tert-butyl 5-(4...

CAS#:837392-67-3

~%

GSK2606414 Structure

GSK2606414

CAS#: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
tert-Butyl 5-bromoindoline-1-carboxylate structure

tert-Butyl 5-br...

CAS#:261732-38-1

~%

GSK2606414 Structure

GSK2606414

CAS#: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
4-Chloro-7-methyl-7H-pyrrolo[2,3-d]pyrimidine structure

4-Chloro-7-meth...

CAS#:7781-10-4

~%

GSK2606414 Structure

GSK2606414

CAS#: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
5-Bromo-4-chloro-7-methyl-7H-pyrrolo[2,3-d]pyrimidine structure

5-Bromo-4-chlor...

CAS#:1266343-30-9

~%

GSK2606414 Structure

GSK2606414

CAS#: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
5-Bromo-7-Methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine structure

5-Bromo-7-Methy...

CAS#:1337532-51-0

~%

GSK2606414 Structure

GSK2606414

CAS#: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

 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
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  • Product Name: GSK2606414
  • Price: $450.0/100mg $900.0/250mg $1800.0/1g
  • Purity: 98.0%
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