General Information of the Drug (ID: M6APDG02204)
Name
GSK2141795
Synonyms
Uprosertib; 1047634-65-0; GSK2141795; UNII-ZXM835LQ5E; Uprosertib (GSK2141795); GSK2141795C; ZXM835LQ5E; GSK795; GSK-2141795; 2-Furancarboxamide, N-[(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-;2-Furancarboxamide, N-[(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-; Uprosertib [USAN:INN]; Uprosertib (USAN/INN); Uprosertib, GSK2141795; SCHEMBL168584; GTPL7902; CHEMBL3137336; MolPort-044-560-307; AXTAPYRUEKNRBA-JTQLQIEISA-N
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Status
Phase 2
Structure
Formula
C18H16Cl2F2N4O2
InChI
1S/C18H16Cl2F2N4O2/c1-26-16(12(19)8-24-26)11-6-15(28-17(11)20)18(27)25-10(7-23)4-9-2-3-13(21)14(22)5-9/h2-3,5-6,8,10H,4,7,23H2,1H3,(H,25,27)/t10-/m0/s1
InChIKey
AXTAPYRUEKNRBA-JTQLQIEISA-N
PubChem CID
51042438
TTD Drug ID
D01NEC
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
RAC-gamma serine/threonine-protein kinase (AKT3)
Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-gamma serine/threonine-protein kinase (AKT3) is a therapeutic target for GSK2141795. The Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) has potential in affecting the response of GSK2141795 through regulating the expression of RAC-gamma serine/threonine-protein kinase (AKT3). [1], [2]
References
Ref 1 HNRNPA2B1 promotes multiple myeloma progression by increasing AKT3 expression via m6A-dependent stabilization of ILF3 mRNA. J Hematol Oncol. 2021 Apr 1;14(1):54. doi: 10.1186/s13045-021-01066-6.
Ref 2 First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors. J Clin Oncol. 2011 Dec 10;29(35):4688-95. doi: 10.1200/JCO.2011.35.5263. Epub 2011 Oct 24.