m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02063)
Name
NS-018
Synonyms
NS-018; ilginatinib; 1239358-86-1; UNII-56R994WX4L; 56R994WX4L; GTPL7839; SCHEMBL14954406; UQTPDWDAYHAZNT-AWEZNQCLSA-N; NS018; ZINC68245917; HY-19631A; AKOS030526348; DB12784; CS-5358; SB16921; 2,6-Pyridinediamine, N2-((1S)-1-(4-fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N6-2-pyrazinyl-; (S)-N2-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N6-(pyrazin-2yl)pyridine-2,6-diamine; (S)-N-(1-(4-Fluorophenyl)ethyl)-4-(1-methyl-1H-pyrazol-4-yl)-N'-(pyrazin-2-yl)pyridine-2,6-diamine
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Status
Phase 1/2
Structure
Formula
C21H20FN7
InChI
1S/C21H20FN7/c1-14(15-3-5-18(22)6-4-15)26-19-9-16(17-11-25-29(2)13-17)10-20(27-19)28-21-12-23-7-8-24-21/h3-14H,1-2H3,(H2,24,26,27,28)/t14-/m0/s1
InChIKey
UQTPDWDAYHAZNT-AWEZNQCLSA-N
PubChem CID
46866319
TTD Drug ID
D00MYW
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.
Janus kinase 2 (JAK-2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for NS-018. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of NS-018 through regulating the expression of Janus kinase 2 (JAK-2). [1], [2]
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for NS-018. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of NS-018 through regulating the expression of Janus kinase 2 (JAK-2). [2], [3]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for NS-018. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of NS-018 through regulating the expression of Janus kinase 2 (JAK-2). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Janus kinase 2 (JAK-2) is a therapeutic target for NS-018. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of NS-018 through regulating the expression of Janus kinase 2 (JAK-2). [2], [4]
References
Ref 1 FTO inhibits UPR(mt)-induced apoptosis by activating JAK2/STAT3 pathway and reducing m6A level in adipocytes. Apoptosis. 2021 Aug;26(7-8):474-487. doi: 10.1007/s10495-021-01683-z. Epub 2021 Jul 1.
Ref 2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2048).
Ref 3 N6-Methyladenosine Methyltransferase METTL3 Promotes Angiogenesis and Atherosclerosis by Upregulating the JAK2/STAT3 Pathway via m6A Reader IGF2BP1. Front Cell Dev Biol. 2021 Dec 7;9:731810. doi: 10.3389/fcell.2021.731810. eCollection 2021.
Ref 4 ALKBH5-HOXA10 loop-mediated JAK2 m6A demethylation and cisplatin resistance in epithelial ovarian cancer. J Exp Clin Cancer Res. 2021 Sep 8;40(1):284. doi: 10.1186/s13046-021-02088-1.