Drug Information

Drug (ID: DG01499) and It's Reported Resistant Information

• Name: AV-412
• Synonyms: 451492-95-8; AV-412 free base; AV-412; AV-412 (free base); UNII-41OXH4FE7B; MP-412; AV412; N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide; N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide; 41OXH4FE7B; CHEMBL2138625; AV-412(MP-412); C27H28ClFN6O; 2-Propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-; N-(4-(3-chloro-4-fluorophenylamino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl)quinazolin-6-yl)acrylamide; 2-Propenamide, N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl)-6-quinazolinyl)-; 2-propenamide,n-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl)-6-quinazolinyl)-; 2-Propenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-; MP-412 free base; SCHEMBL1818495; AV-412 free base;MP-412; DTXSID10196403; EX-A755; SYN1012; BCPP000375; HMS3244M15; HMS3244M16; HMS3244N15; BCP01955; 3459AH; BDBM50468245; HY-10346A; MFCD16038939; NSC799340; ZINC22453472; AKOS027251058; BCP9000342; NSC-799340; NCGC00263195-01; NCGC00263195-04; AS-16187; B3236; FT-0700308; A872418; J-523023; Q27258451; N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-methyl-3-(4-methyl-1-piperazinyl)-1-butyn-1-yl]-6-quinazolinyl]-2-propenamide
• Target: .; NOUNIPROTAC; [1]
• Formula: 7
• IsoSMILES: CC(C)(C#CC1=CC2=C(C=C1NC(=O)C=C)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)N4CCN(CC4)C
• InChI: InChI=1S/C27H28ClFN6O/c1-5-25(36)33-23-16-20-24(30-17-31-26(20)32-19-6-7-22(29)21(28)15-19)14-18(23)8-9-27(2,3)35-12-10-34(4)11-13-35/h5-7,14-17H,1,10-13H2,2-4H3,(H,33,36)(H,30,31,32)
• InChIKey: ZAJXXUDARPGGOC-UHFFFAOYSA-N
• PubChem CID: 9806229
• DrugBank ID: DB06021

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: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Missense mutation; p.T790M (c.2369C>T)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: A431 cells; Skin; Homo sapiens (Human); CVCL_0037
• In Vitro Model: TE8 cells; Esophageal; Homo sapiens (Human); CVCL_1766
• In Vitro Model: A4 cells; N.A.; Mus musculus (Mouse); CVCL_F962
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: 3H-thymidine incorporation assay
• Mechanism Description: The missense mutation p.T790M (c.2369C>T) in gene EGFR cause the sensitivity of AV-412 by aberration of the drug's therapeutic target

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Molecule Alteration: Missense mutation; p.L858R (c.2573T>G)
• Sensitive Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: A431 cells; Skin; Homo sapiens (Human); CVCL_0037
• In Vitro Model: TE8 cells; Esophageal; Homo sapiens (Human); CVCL_1766
• In Vitro Model: A4 cells; N.A.; Mus musculus (Mouse); CVCL_F962
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: 3H-thymidine incorporation assay
• Mechanism Description: The missense mutation p.L858R (c.2573T>G) in gene EGFR cause the sensitivity of AV-412 by aberration of the drug's therapeutic target

References

• Ref 1: Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitorCancer Sci. 2007 Dec;98(12):1977-84. doi: 10.1111/j.1349-7006.2007.00613.x. Epub 2007 Sep 18.