General Information of the Drug (ID: M6ADRUG0093)
Name
Sunitinib
Synonyms
Sunitinib; 557795-19-4; Sutent; SU11248; Sunitinib Base; SU-11248; Su-011248; SU 11248; 342641-94-5; (Z)-N-(2-(Diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide; UNII-V99T50803M; N-(2-(Diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; CHEMBL535; CHEBI:38940; SU011248; NSC750690; NSC-750690; V99T50803M; sunitinibum; Sunitinib (INN); 1H-Pyrrole-3-carboxamide, N-(2-(diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-; n-(2-(diethylamino)ethyl)-5-((z)-(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-2,4-dimethyl-1h-pyrrole-3-carboxamide; Sunitinib (free base); NSC-736511; Sunitinib [INN:BAN]; 5-(5-FLUORO-2-OXO-1,2-DIHYDRO-INDOL-3-YLIDENEMETHYL)-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXYLIC ACID (2-DIETHYLAMINO-ETHYL)-AMIDE; C22H27FN4O2; MFCD09260778; HSDB 7932; (Z)-Sunitinib; 1H-Pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-; 5-(5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylamino-ethyl)-amide; 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylamino-ethyl)-amide; n-[2-(diethylamino)ethyl]-5-[(z)-(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide; Sutent (free base); KS-5022; SCHEMBL8081; BDBM4814; GTPL5713; QCR-67; Sutent, Sunitinib, SU11248; CHEBI:91430; EX-A553; BCPP000057; K00588a; AOB87111; ZINC3964325; HY-10255A; NSC800937; s7781; AKOS015908193; AKOS025312424; CCG-268638; CS-1670; DB01268; NSC 736511; NSC 750690; NSC-800937; NCGC00164631-02; NCGC00164631-04; BD164426; Q572; 1,2,4,5-tetramethylpyrrole-3-carboxamide; AM20090630; 95S194; D08552; J90060; AB01273976-01; AB01273976-02; AB01273976_04; A822143; A830806; Q417542; SR-00000000005; SR-00000000005-2; Q27163278; Z2568722545; 1H-Pyrrole-3-carboxamide,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-; 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid(2-diethylamino-ethyl)-amide; N-[2-(Diethylamino)ethyl]-5-(2-oxo-5-fluoroindoline-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo
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Status Approved [1]
Structure
Formula
C22H27FN4O2
InChI
InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChIKey
WINHZLLDWRZWRT-ATVHPVEESA-N
PubChem CID
5329102
TTD Drug ID
D0R0MW
DrugBank ID
DB01268
Full List of m6A Targets Related to This Drug
TNF receptor-associated factor 1 (TRAF1)
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 renal cell carcinoma, overexpression of TNF receptor-associated factor 1 (TRAF1) promotes sunitinib resistance by modulating apoptotic and angiogenic pathways in a METTL14-dependent manner.
Responsed Disease Renal cell carcinoma ICD-11: 2C90
Target Regulator Methyltransferase-like 14 (METTL14) WRITER
Target Regulation Up regulation
Cell Process RNA stability
Cell apoptosis
In-vitro Model OS-RC-2 Clear cell renal cell carcinoma Homo sapiens CVCL_1626
HUVEC-C Normal Homo sapiens CVCL_2959
786-O Renal cell carcinoma Homo sapiens CVCL_1051
In-vivo Model For the xenograft tumor model, approximately 1 × 106 ccRCC cells suspended in 100 uL PBS were subcutaneously inoculated in the right flank of 5-week-old BALB/c nude mice. For the ccRCC orthotopic implantation model, approximately 1 × 106 ccRCC cells suspended in 30 uL Matrigel were injected under the renal capsule of 5-week-old BALB/c nude mice. After 6 weeks, the anesthetized mice were intraperitoneally injected with D-luciferin (Yeason) and imaged using an in vivo imaging system to detect tumor growth and metastasis. For the lung metastasis model, approximately 5 × 105 ccRCC cells suspended in PBS were injected into the tail vein of 5-week-old mice. After 6-8 weeks, mice were anesthetized and lung metastasis was imaged as above.
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: 5713).
Ref 2 N(6)-methyladenosine-modified TRAF1 promotes sunitinib resistance by regulating apoptosis and angiogenesis in a METTL14-dependent manner in renal cell carcinoma. Mol Cancer. 2022 May 10;21(1):111. doi: 10.1186/s12943-022-01549-1.