Drug Information

Drug (ID: DG01611) and It's Reported Resistant Information

• Name: EPZ005687
• Synonyms: EPZ005687; 1396772-26-1; EPZ-005687; 1-cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide; EPZ 005687; 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide; EZH2 Inhibitor, EPZ005687; UNII-GQ4LD5KG1E; GQ4LD5KG1E; GTPL8387; SCHEMBL12684069; AOB1761; DTXSID80733849; EX-A429; CHEBI:124922; EPZ 5687 [WHO-DD]; C32H37N5O3; BCP07899; EPZ 5687; EPZ-5687; WFC77226; 2398AH; MFCD25372029; NSC783332; s7004; ZINC98043813; AKOS026750254; CCG-269957; CS-1215; NSC-783332; SB19050; NCGC00351604-01; NCGC00351604-09; NCGC00351604-12; AC-32708; AS-16367; DA-34778; HY-15555; QC-11445; FT-0700189; Q27077206; 1-Cyclopentyl-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-6-{4-[(morpholin-4-yl)methyl]phenyl}-1H-indazole-4-carboxamide; 1H-Indazole-4-carboxamide, 1-cyclopentyl-N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-6-(4-(4-morpholinylmethyl)phenyl)-; cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide
• Indication:
  In total 2 Indication(s)
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Investigative; [1]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Investigative; [1]
• Target: Serine/threonine-protein kinase ATR (FRP1); ATR_HUMAN; [1]
• Formula: 7
• IsoSMILES: CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC=C(C=C4)CN5CCOCC5)C6CCCC6)C
• InChI: InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39)
• InChIKey: ZOIBZSZLMJDVDQ-UHFFFAOYSA-N
• PubChem CID: 60160561
• ChEBI ID: CHEBI:124922
• TTD Drug ID: D06DMQ

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Lymphoma [ICD-11: 2A90- 2A85]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Histone-lysine N-methyltransferase EZH2 (EZH2) [1]

• Molecule Alteration: Missense mutation; p.Y641F (c.1922A>T)
• Sensitive Disease: Lymphoma [ICD-11: 2A90- 2A85]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: 293 cells; Kidney; Homo sapiens (Human); N.A.
• Experiment for Drug Resistance: Determination of inhibitor IC50 values in the PMT panel assay
• Mechanism Description: The missense mutation p.Y641F (c.1922A>T) in gene EZH2 cause the sensitivity of EPZ005687 by aberration of the drug's therapeutic target

References

• Ref 1: A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cellsNat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30.