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Uprosertib

  Cat. No.:  DC8033   Featured
Chemical Structure
1047634-65-0
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More than 5000 active chemicals with high quality for research!
Field of application
Uprosertib is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1047634-65-0
Chemical Name: N-((S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide
SMILES: FC1=CC=C(C[C@@H](CN)NC(C2=CC(C3=C(Cl)C=NN3C)=C(Cl)O2)=O)C=C1F
Formula: C18H16Cl2F2N4O2
M.Wt: 428.06
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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