Drug Information

Drug (ID: DG01572) and It's Reported Resistant Information

• Name: WZ4002
• Synonyms: WZ4002; 1213269-23-8; WZ-4002; N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide; WZ 4002; UNII-6BQ432Z61M; CHEBI:61400; CHEMBL1229592; 6BQ432Z61M; N-(3-((5-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide; N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide; N-{3-[(5-chloro-2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)oxy]phenyl}prop-2-enamide; SMR001913510; SCHEMBL93699; MLS003230945; MLS006011213; AMY370; GTPL9176; QCR-55; DTXSID30153230; EX-A416; HMS3265O15; HMS3265O16; HMS3265P15; HMS3265P16; HMS3654C16; BCP02515; BDBM50383274; NSC755927; s1173; ZINC52509385; AKOS025401946; CCG-264847; CS-0167; NSC-755927; SB19360; NCGC00263144-01; NCGC00263144-02; NCGC00263144-11; AC-27472; AS-19387; DA-47168; HY-12026; N-(3-((5-chloro-2-((2-methoxy-4-(4-methyl-1-piperazinyl)phenyl)amino)-4-pyrimidinyl)oxy)phenyl)acrylamide; N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide; WZ4002, >=98% (HPLC); FT-0730384; SW219315-1; X7482; EC-000.2280; A25634; J-004480; J-523322; Q27089236; N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazine-1-yl)phenylamino)pyrimidin-4yloxy)phenyl)acrylam; N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide HBr
• Indication:
  In total 1 Indication(s)
  Lung cancer [ICD-11: 2C25]; Phase 3; [1]
• Target: Epidermal growth factor receptor (EGFR); EGFR_HUMAN; [1]
• Formula: 8
• IsoSMILES: CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)OC4=CC=CC(=C4)NC(=O)C=C)Cl)OC
• InChI: InChI=1S/C25H27ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h4-9,14-16H,1,10-13H2,2-3H3,(H,28,33)(H,27,29,30)
• InChIKey: ITTRLTNMFYIYPA-UHFFFAOYSA-N
• PubChem CID: 44607530

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

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]

• Molecule Alteration: Missense mutation; p.L755S (c.2263_2264delCTinsAG)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HEK293 cells; Kidney; Homo sapiens (Human); CVCL_0045
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: MTS assay
• Mechanism Description: The missense mutation p.L755S (c.2263_2264delCTinsAG) in gene ERBB2 cause the sensitivity of WZ4002 by aberration of the drug's therapeutic target

Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]

• Molecule Alteration: Missense mutation; p.L755P (c.2264T>C)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HEK293 cells; Kidney; Homo sapiens (Human); CVCL_0045
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: MTS assay
• Mechanism Description: The missense mutation p.L755P (c.2264T>C) in gene ERBB2 cause the sensitivity of WZ4002 by aberration of the drug's therapeutic target

Key Molecule: Receptor tyrosine-protein kinase erbB-2 (ERBB2) [1]

• Molecule Alteration: Missense mutation; p.T798M (c.2393_2394delCAinsTG)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HEK293 cells; Kidney; Homo sapiens (Human); CVCL_0045
• In Vitro Model: Ba/F3 cells; Colon; Homo sapiens (Human); CVCL_0161
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: MTS assay
• Mechanism Description: The missense mutation p.T798M (c.2393_2394delCAinsTG) in gene ERBB2 cause the sensitivity of WZ4002 by aberration of the drug's therapeutic target

References

• Ref 1: Differential sensitivity of ERBB2 kinase domain mutations towards lapatinibPLoS One. 2011;6(10):e26760. doi: 10.1371/journal.pone.0026760. Epub 2011 Oct 28.