m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02115)
Name
VS-5584
Synonyms
5-(9-Isopropyl-8-methyl-2-morpholino-9H-purin-6-yl)pyrimidin-2-amine; 1246560-33-7; VS-5584 (SB2343); UNII-W71J4X250V; SB-2343; SB2343; CHEMBL3393066; W71J4X250V; 5-(8-methyl-2-morpholin-4-yl-9-propan-2-ylpurin-6-yl)pyrimidin-2-amine; C17H22N8O; QYBGBLQCOOISAR-UHFFFAOYSA-N; SCHEMBL539098; GTPL8382; EX-A288; DTXSID10677328; MolPort-035-757-944; HMS3652B16; BCP08247; 2797AH; ZINC95644685; s7016; VS5584; BDBM50059635; AKOS024465057; 5-(9-isopropyl-8-methyl-2-morpholin-4-yl-9H-purin-6-yl)-pyrimidin-2-ylamine; SB16877
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Status
Phase 1
Structure
Formula
C17H22N8O
InChI
1S/C17H22N8O/c1-10(2)25-11(3)21-14-13(12-8-19-16(18)20-9-12)22-17(23-15(14)25)24-4-6-26-7-5-24/h8-10H,4-7H2,1-3H3,(H2,18,19,20)
InChIKey
QYBGBLQCOOISAR-UHFFFAOYSA-N
PubChem CID
46912230
TTD Drug ID
D0U3DP
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.
Mammalian target of rapamycin complex 1 (mTORC1)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mammalian target of rapamycin complex 1 (mTORC1) is a therapeutic target for VS-5584. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of VS-5584 through regulating the expression of Mammalian target of rapamycin complex 1 (mTORC1). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mammalian target of rapamycin complex 1 (mTORC1) is a therapeutic target for VS-5584. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of VS-5584 through regulating the expression of Mammalian target of rapamycin complex 1 (mTORC1). [2], [3]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mammalian target of rapamycin complex 1 (mTORC1) is a therapeutic target for VS-5584. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of VS-5584 through regulating the expression of Mammalian target of rapamycin complex 1 (mTORC1). [2], [3]
RNA-binding motif protein 15 (RBM15)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mammalian target of rapamycin complex 1 (mTORC1) is a therapeutic target for VS-5584. The RNA-binding motif protein 15 (RBM15) has potential in affecting the response of VS-5584 through regulating the expression of Mammalian target of rapamycin complex 1 (mTORC1). [2], [3]
RNA-binding motif protein 15B (RBM15B)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mammalian target of rapamycin complex 1 (mTORC1) is a therapeutic target for VS-5584. The RNA-binding motif protein 15B (RBM15B) has potential in affecting the response of VS-5584 through regulating the expression of Mammalian target of rapamycin complex 1 (mTORC1). [2], [3]
Wilms tumor 1-associating protein (WTAP)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Mammalian target of rapamycin complex 1 (mTORC1) is a therapeutic target for VS-5584. The Wilms tumor 1-associating protein (WTAP) has potential in affecting the response of VS-5584 through regulating the expression of Mammalian target of rapamycin complex 1 (mTORC1). [2], [3]
Serine/threonine-protein kinase mTOR (mTOR)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for VS-5584. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of VS-5584 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [4], [5]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for VS-5584. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of VS-5584 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [5], [6]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for VS-5584. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of VS-5584 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [5], [7]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for VS-5584. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of VS-5584 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [5], [8]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Serine/threonine-protein kinase mTOR (mTOR) is a therapeutic target for VS-5584. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of VS-5584 through regulating the expression of Serine/threonine-protein kinase mTOR (mTOR). [4], [5]
Target of rapamycin complex 2 MAPKAP1 (MTORC2)
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Target of rapamycin complex 2 MAPKAP1 (MTORC2) is a therapeutic target for VS-5584. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of VS-5584 through regulating the expression of Target of rapamycin complex 2 MAPKAP1 (MTORC2). [9], [10]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Target of rapamycin complex 2 MAPKAP1 (MTORC2) is a therapeutic target for VS-5584. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of VS-5584 through regulating the expression of Target of rapamycin complex 2 MAPKAP1 (MTORC2). [9], [10]
References
Ref 1 Omeprazole improves chemosensitivity of gastric cancer cells by m6A demethylase FTO-mediated activation of mTORC1 and DDIT3 up-regulation. Biosci Rep. 2021 Jan 29;41(1):BSR20200842. doi: 10.1042/BSR20200842.
Ref 2 Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation. J Clin Invest. 2019 Apr 16;129(6):2542-2554. doi: 10.1172/JCI126859.
Ref 3 mTORC1-chaperonin CCT signaling regulates m(6)A RNA methylation to suppress autophagy. Proc Natl Acad Sci U S A. 2021 Mar 9;118(10):e2021945118. doi: 10.1073/pnas.2021945118.
Ref 4 Targeting ATF4-dependent pro-survival autophagy to synergize glutaminolysis inhibition. Theranostics. 2021 Jul 25;11(17):8464-8479. doi: 10.7150/thno.60028. eCollection 2021.
Ref 5 Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220. doi: 10.1371/journal.pone.0087220. eCollection 2014.
Ref 6 The m6A methyltransferase METTL14 inhibits the proliferation, migration, and invasion of gastric cancer by regulating the PI3K/AKT/mTOR signaling pathway. J Clin Lab Anal. 2021 Mar;35(3):e23655. doi: 10.1002/jcla.23655. Epub 2020 Dec 12.
Ref 7 Methyltransferase-like 3 promotes the progression of lung cancer via activating PI3K/AKT/mTOR pathway. Clin Exp Pharmacol Physiol. 2022 Jul;49(7):748-758. doi: 10.1111/1440-1681.13647. Epub 2022 May 23.
Ref 8 YTHDF1 promotes hepatocellular carcinoma progression via activating PI3K/AKT/mTOR signaling pathway and inducing epithelial-mesenchymal transition. Exp Hematol Oncol. 2021 Jun 4;10(1):35. doi: 10.1186/s40164-021-00227-0.
Ref 9 m(6)A mRNA methylation regulates AKT activity to promote the proliferation and tumorigenicity of endometrial cancer. Nat Cell Biol. 2018 Sep;20(9):1074-1083. doi: 10.1038/s41556-018-0174-4. Epub 2018 Aug 27.
Ref 10 Dual mTORC1 and mTORC2 inhibitor Palomid 529 penetrates the blood-brain barrier without restriction by ABCB1 and ABCG2. Int J Cancer. 2013 Sep 1;133(5):1222-33. doi: 10.1002/ijc.28126. Epub 2013 Apr 1.