Uprosertib

Modify Date: 2024-01-03 16:32:07

Uprosertib Structure
Uprosertib structure
Common Name Uprosertib
CAS Number 1047634-65-0 Molecular Weight 429.24800
Density N/A Boiling Point N/A
Molecular Formula C18H16Cl2F2N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Uprosertib


Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

 Names

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

 Uprosertib Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C18H16Cl2F2N4O2
Molecular Weight 429.24800
Exact Mass 428.06200
PSA 86.08000
LogP 4.65610
Storage condition -20℃

 Synonyms

Uprosertib
GSK2141795
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