937174-76-0 Usage
Uses
Used in Pharmaceutical Industry:
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol is used as a pharmaceutical compound for its potential therapeutic applications. Its complex structure and multiple functional groups may contribute to its interaction with biological targets, making it a candidate for the development of new drugs.
Used in Research Applications:
In the field of scientific research, 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol can be utilized in various assays and experiments to study its interactions with biological systems. Its unique structure and functional groups may provide insights into the development of new therapeutic agents and contribute to a better understanding of molecular mechanisms in disease processes.
Used in Drug Design and Development:
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol's structural features make it a valuable asset in drug design and development. Its potential to interact with various biological targets can be explored to create new drugs with improved efficacy and selectivity, ultimately benefiting patients in need of novel treatment options.
Used in Chemical Synthesis:
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol can also be used as a starting material or intermediate in the synthesis of other complex organic molecules. Its unique structure and functional groups can be further modified to create a variety of new compounds with different properties and applications.
Biochem/physiol Actions
GSK690693 is an ATP competitive, potent pan-AKT kinase inhibitor with IC50 values of 2, 13, and 9 nM against AKT1, 2, and 3, respectively.
References
1) Rhodes et al. (2008), Characterization of an Akt kinase inhibitor with potent pharmacodynamics and antitumor activity; Cancer Res., 68 2366
2) Crouthamel et al. (2009), Mechanism and management of AKT inhibitor-induced hyperglycemia; Clin. Cancer Res., 15 217
Check Digit Verification of cas no
The CAS Registry Mumber 937174-76-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,3,7,1,7 and 4 respectively; the second part has 2 digits, 7 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 937174-76:
(8*9)+(7*3)+(6*7)+(5*1)+(4*7)+(3*4)+(2*7)+(1*6)=200
200 % 10 = 0
So 937174-76-0 is a valid CAS Registry Number.
937174-76-0Relevant academic research and scientific papers
METHODS OF USE FOR INHIBITORS OF AKT ACTIVITY
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, (2008/12/04)
Invented is the use of 1 H-imidazo[4,5-c]pyridin-2-yl compounds in the treatment of specified cancers.
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3- piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase
Heerding, Dirk A.,Rhodes, Nelson,Leber, Jack D.,Clark, Tammy J.,Keenan, Richard M.,Lafrance, Louis V.,Li, Mei,Safonov, Igor G.,Takata, Dennis T.,Venslavsky, Joseph W.,Yamashita, Dennis S.,Choudhry, Anthony E.,Copeland, Robert A.,Lai, Zhihong,Schaber, Michael D.,Tummino, Peter J.,Strum, Susan L.,Wood, Edgar R.,Duckett, Derek R.,Eberwein, Derek,Knick, Victoria B.,Lansing, Timothy J.,McConnell, Randy T.,Zhang, ShuYun,Minthorn, Elisabeth A.,Concha, Nestor O.,Warren, Gregory L.,Kumar, Rakesh
experimental part, p. 5663 - 5679 (2009/08/07)
Overexpression of AKT has an antiapoptotic effect in many cell types, and expression of dominant negative AKT blocks the ability of a variety of growth factors to promote survival. Therefore, inhibitors of AKT kinase activity might be useful as monotherapy for the treatment of tumors with activated AKT. Herein, we describe our lead optimization studies culminating in the discovery of compound 3g (GSK690693). Compound 3g is a novel ATP competitive, pan-AKT kinase inhibitor with IC50 values of 2, 13, and 9 nM against AKT1, 2, and 3, respectively. An X-ray cocrystal structure was solved with 3g and the kinase domain of AKT2, confirming that 3g bound in the ATP binding pocket. Compound 3g potently inhibits intracellular AKT activity as measured by the inhibition of the phosphorylation levels of GSK3β. Intraperitoneal administration of 3g in immunocompromised mice results in the inhibition of GSK3β phosphorylation and tumor growth in human breast carcinoma (BT474) xenografts.
