m6A-centered Drug Response Information

General Information of the Drug (ID: M6ADRUG0105)
Name
Everolimus
Synonyms
001, RAD; 40-O-(2-hydroxyethyl)-rapamycin; 40-O-(2-Hydroxyethyl)rapamycin; Afinitor; Certican; Everolimus; RAD; RAD 001; RAD, SDZ; RAD001; SDZ RAD; SDZ-RAD; Zortress; 159351-69-6; 42-O-(2-Hydroxyethyl)rapamycin; Votubia; Afinitor Disperz; CHEBI:68478; RAD-001; Rapamycin, 42-O-(2-hydroxyethyl)-; UNII-9HW64Q8G6G; 9HW64Q8G6G; NCGC00167512-01; Everolimus (RAD001); (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-3-{(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl}-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone; (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,35R)-1,18-dihydroxy-12-{(2R)-1-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl]propan-2-yl}-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.0(4,9)]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone; everolimusum; NSC733504; Everolimus solution; Everolimus (INN); SDZRAD; XIENCE V; Everolimus - RAD001; SCHEMBL4378; DSSTox_CID_20599; DSSTox_RID_79508; NVP-RAD001; DSSTox_GSID_40599; Everolimus [USAN:INN:BAN]; NVP-RAD-001; Everolimus, analytical standard; GTPL5889; RAD-001C; CHEMBL1908360; DTXSID0040599; HSDB 8255; RAD 666; RAD-666; Everolimus; RAD001; SDZ-RAD; C53H83NO14; 42-O-(2-Hydroxyethyl)-rapamycin; EX-A2057; Tox21_112510; BDBM50088378; AKOS015850977; ZINC169677008; CS-0064; DB01590; (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-Dihydroxy-12-((1R)-2-((1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl)-1-methylethyl)-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo(30.3.1.0(sup 4,9))hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentaone; (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-Dihydroxy-12-((1R)-2-((1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl)-1-methylethyl)-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo(30.3.1.04,9)hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentaone; (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hexadecahydro-9,27-dihydroxy-3-((1R)-2-((1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxycyclohexyl)-1-methylethyl)-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone; AS-16971; HY-10218; CAS-159351-69-6; V2036; Everolimus solution, 1.0 mg/ml in acetonitrile; 351E696; Q421052; Q-101413; BRD-K13514097-001-01-2; BRD-K13514097-001-05-3; dihydroxy-[(1R)-2-[(1S,3R,4R)-4-(2-hydroxyethoxy)-3-methoxy-cyclohexyl]-1-methyl-ethyl]-dimethoxy-hexamethyl-[?]pentone; Everolimus solution, 1.0 mg/mL in acetonitrile, ampule of 1 mL, certified reference material
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Status Approved [1]
Structure
3D MOL
2D MOL
Formula
C53H83NO14
InChI
InChI=1S/C53H83NO14/c1-32-16-12-11-13-17-33(2)44(63-8)30-40-21-19-38(7)53(62,68-40)50(59)51(60)54-23-15-14-18-41(54)52(61)67-45(35(4)28-39-20-22-43(66-25-24-55)46(29-39)64-9)31-42(56)34(3)27-37(6)48(58)49(65-10)47(57)36(5)26-32/h11-13,16-17,27,32,34-36,38-41,43-46,48-49,55,58,62H,14-15,18-26,28-31H2,1-10H3/b13-11+,16-12+,33-17+,37-27+/t32-,34-,35-,36-,38-,39+,40+,41+,43-,44+,45+,46-,48-,49+,53-/m1/s1
InChIKey
HKVAMNSJSFKALM-GKUWKFKPSA-N
PubChem CID
6442177
TTD Drug ID
D0K3QS
DrugBank ID
DB01590
Full List of m6A Targets Related to This Drug
miR-17-92
 Target Info 
In total 1 item(s) under this target gene
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene [2]
Response Summary In gastric cancer, m6A facilitated processing of pri-miR-17-92 into the miR-17-92 cluster through an m6A/DGCR8-dependent mechanism. METTL3-high tumors showed preferred sensitivity to an mTOR inhibitor, everolimus.
Responsed Disease Gastric cancer ICD-11: 2B72
 Disease Info 
Target Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
Target Regulation Up regulation
Pathway Response mTOR signaling pathway hsa04150
PI3K-Akt signaling pathway hsa04151
Cell Process miRNA maturation
In-vitro Model MKN45 Gastric adenocarcinoma Homo sapiens CVCL_0434
HGC-27 Gastric carcinoma Homo sapiens CVCL_1279
AGS Gastric adenocarcinoma Homo sapiens CVCL_0139
In-vivo Model For subcutaneous xenograft models, 0.1 mL of cell suspension containing 106 cells were injected subcutaneously into the right flank of mice (n = 6 for each group).
References
Ref 1 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. (Ligand id: 5889).
Ref 2 N(6)-methyladenosine-dependent pri-miR-17-92 maturation suppresses PTEN/TMEM127 and promotes sensitivity to everolimus in gastric cancer. Cell Death Dis. 2020 Oct 9;11(10):836. doi: 10.1038/s41419-020-03049-w.