1047634-65-0

1047634-65-0 structure

Name: Uprosertib
Chemical Name: N-[(2S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)furan-2-carboxamide
CAS Number: 1047634-65-0
Molecular Formula: C₁₈H₁₆Cl₂F₂N₄O₂
Molecular Weight: 429.24800
Catalog: Signaling Pathways PI3K/Akt/mTOR Akt
Create Date: 2017-04-14 02:49:26
Modify Date: 2024-01-03 16:32:07
Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

Name	N-[(2S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)furan-2-carboxamide
Synonyms	Uprosertib GSK2141795

Description	Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
Related Catalog	Signaling Pathways >> PI3K/Akt/mTOR >> Akt Research Areas >> Cancer
Target	Akt1:180 nM (IC50) Akt2:328 nM (IC50) Akt3:38 nM (IC50) CDK7:2100 nM (IC50) ROCK1:1570 nM (IC50) ROCK2:1850 nM (IC50)
In Vitro	Uprosertib (GSK2141795) inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. Uprosertib potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind Uprosertib (GSK2141795) in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].
References	[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800. [2]. Jacobsen K, et al. Convergent Akt activation drives acquired EGFR inhibitor resistance in lung cancer. Nat Commun. 2017 Sep 4;8(1):410.