General Information of the Drug (ID: M6APDG02649)
Name
CYC116
Synonyms
693228-63-6; CYC-116; CYC116; CHEMBL482967; Kinome_636; 4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine; 4-Methyl-5-(2-((4-morpholinophenyl)amino)-pyrimidin-4-yl)thiazol-2-amine; 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine; 4-methyl-5-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)thiazol-2-amine; 2uue; CYC 116; GPSZYOIFQZPWEJ-UHFFFAOYSA-N; 2c5t; AC1O4WKE; MLS006011244; SCHEMBL2074998; SYN1034; EX-A753; CYC-116/CYC116; MolPort-009-679-476; HMS3244O12; HMS3244P11; BCPP000273
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Status
Phase 1
Structure
Formula
C18H20N6OS
InChI
1S/C18H20N6OS/c1-12-16(26-17(19)21-12)15-6-7-20-18(23-15)22-13-2-4-14(5-3-13)24-8-10-25-11-9-24/h2-7H,8-11H2,1H3,(H2,19,21)(H,20,22,23)
InChIKey
GPSZYOIFQZPWEJ-UHFFFAOYSA-N
PubChem CID
6420138
TTD Drug ID
D0CY1B
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.
Aurora kinase B (AURKB)
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Aurora kinase B (AURKB) is a therapeutic target for CYC116. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of CYC116 through regulating the expression of Aurora kinase B (AURKB). [1], [2]
References
Ref 1 ALKBH5 promotes the proliferation of renal cell carcinoma by regulating AURKB expression in an m(6)A-dependent manner. Ann Transl Med. 2020 May;8(10):646. doi: 10.21037/atm-20-3079.
Ref 2 Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010 Dec 1;70(23):9846-54. doi: 10.1158/0008-5472.CAN-10-3001. Epub 2010 Oct 8.