m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00312)
Name
R-1487
Synonyms
449811-92-1; 6-(2,4-difluorophenoxy)-8-methyl-2-((tetrahydro-2H-pyran-4-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one; UNII-IO0DCY55NQ; R-1487; IO0DCY55NQ; CHEMBL1230122; 6-(2,4-difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-Pyrido[2,3-d]pyrimidin-7(8H)-one; 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2h-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8h)-one; Kinome_3762; SCHEMBL5120612; KKKRKRMVJRHDMG-UHFFFAOYSA-N; HMS3401C13; BDBM50341342; ZINC58633224; AKOS027420928; NCGC00262195-02; KB-80224; ACM449811921
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Status
Discontinued in Phase 1
Structure
Formula
C19H18F2N4O3
InChI
1S/C19H18F2N4O3/c1-25-17-11(10-22-19(24-17)23-13-4-6-27-7-5-13)8-16(18(25)26)28-15-3-2-12(20)9-14(15)21/h2-3,8-10,13H,4-7H2,1H3,(H,22,23,24)
InChIKey
KKKRKRMVJRHDMG-UHFFFAOYSA-N
PubChem CID
11406590
TTD Drug ID
D04YHW
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.
Stress-activated protein kinase 2a (p38 alpha)
Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Stress-activated protein kinase 2a (p38 alpha) is a therapeutic target for R-1487. The Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) has potential in affecting the response of R-1487 through regulating the expression of Stress-activated protein kinase 2a (p38 alpha). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Stress-activated protein kinase 2a (p38 alpha) is a therapeutic target for R-1487. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of R-1487 through regulating the expression of Stress-activated protein kinase 2a (p38 alpha). [2], [3]
YTH domain-containing family protein 3 (YTHDF3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Stress-activated protein kinase 2a (p38 alpha) is a therapeutic target for R-1487. The YTH domain-containing family protein 3 (YTHDF3) has potential in affecting the response of R-1487 through regulating the expression of Stress-activated protein kinase 2a (p38 alpha). [1], [2]
References
Ref 1 N6-methyladenosine reader YTH N6-methyladenosine RNA binding protein 3 or insulin like growth factor 2 mRNA binding protein 2 knockdown protects human bronchial epithelial cells from hypoxia/reoxygenation injury by inactivating p38 MAPK, AKT, ERK1/2, and NF-KappaB pathways. Bioengineered. 2022 May;13(5):11973-11986. doi: 10.1080/21655979.2021.1999550.
Ref 2 Pharmacological inhibitors of MAPK pathways. Trends Pharmacol Sci. 2002 Jan;23(1):40-5. doi: 10.1016/s0165-6147(00)01865-4.
Ref 3 m(6)A methyltransferase METTL3 suppresses colorectal cancer proliferation and migration through p38/ERK pathways. Onco Targets Ther. 2019 Jun 4;12:4391-4402. doi: 10.2147/OTT.S201052. eCollection 2019.