General Information of the Drug (ID: M6APDG02439)
Name
RG-13022
Synonyms
RG-13022; RG 13022; CHEMBL67027; NSC666257; (Z)-3-(3,4-Dimethoxy-phenyl)-2-pyridin-3-yl-acrylonitrile; 136831-48-6; DBGZNJVTHYFQJI-RIYZIHGNSA-N; 149286-90-8; Tyrphostin RG13022; AC1NV4OE; SCHEMBL241869; SCHEMBL1959494; CHEBI:93448; MolPort-009-019-306; BDBM50039091; ZINC37858694; HSCI1_000158; AKOS032947325; NSC-666257; NCGC00018297-02; NCGC00018297-01; J-006919; BRD-K82688027-001-01-5; 3-(3,4-Dimethoxyphenyl)-2-(3-pyridinyl)acrylonitrile; (Z)-3-(3,4-dimethoxyphenyl)-2-pyridin-3-ylprop-2-enenitrile
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Status
Terminated
Structure
Formula
C16H14N2O2
InChI
1S/C16H14N2O2/c1-19-15-6-5-12(9-16(15)20-2)8-14(10-17)13-4-3-7-18-11-13/h3-9,11H,1-2H3/b14-8+
InChIKey
DBGZNJVTHYFQJI-RIYZIHGNSA-N
PubChem CID
5468216
TTD Drug ID
D03WTT
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.
Platelet-derived growth factor receptor alpha (PDGFRA)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Platelet-derived growth factor receptor alpha (PDGFRA) is a therapeutic target for RG-13022. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of RG-13022 through regulating the expression of Platelet-derived growth factor receptor alpha (PDGFRA). [1], [2]
Platelet-derived growth factor receptor beta (PDGFRB)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Platelet-derived growth factor receptor beta (PDGFRB) is a therapeutic target for RG-13022. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of RG-13022 through regulating the expression of Platelet-derived growth factor receptor beta (PDGFRB). [3], [4]
References
Ref 1 METTL3-mediated N (6)-methyladenosine modification governs pericyte dysfunction during diabetes-induced retinal vascular complication. Theranostics. 2022 Jan 1;12(1):277-289. doi: 10.7150/thno.63441. eCollection 2022.
Ref 2 Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15. doi: 10.1021/jm058033i.
Ref 3 Mutant NPM1-Regulated FTO-Mediated m(6)A Demethylation Promotes Leukemic Cell Survival via PDGFRB/ERK Signaling Axis. Front Oncol. 2022 Feb 8;12:817584. doi: 10.3389/fonc.2022.817584. eCollection 2022.
Ref 4 Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones. Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. doi: 10.1016/j.bmc.2006.12.011. Epub 2006 Dec 12.