Drug Information

Drug (ID: DG01602) and It's Reported Resistant Information

• Name: AGI-5198
• Synonyms: AGI-5198; 1355326-35-0; IDH-C35; N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide; AGI 5198; AGI-5198(IDH C35); N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-o-tolylacetamide; CHEMBL2180727; AGI5198; N-cyclohexyl-2-(3-fluoro-N-[2-(2-methylimidazol-1-yl)acetyl]anilino)-2-(2-methylphenyl)acetamide; AGI-5198 (IDH-C35); MLS006010252; GTPL9240; SCHEMBL15118942; C27H31FN4O2; AOB5947; DTXSID30718166; EX-A171; QCR-214; HMS3653K15; HMS3865J13; AMY24200; BCP07382; BDBM50400272; MFCD24848688; NSC773096; s7185; AKOS026674117; CCG-269371; CS-1429; NSC-773096; SB19576; NCGC00347934-01; NCGC00347934-09; BS-14968; DA-35355; HY-18082; SMR004701328; FT-0768624; SW220036-1; X5817; A854356; Q27074345; S900006220; N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamide
• Target: .; NOUNIPROTAC; [1]
• Formula: 7
• IsoSMILES: CC1=CC=CC=C1C(C(=O)NC2CCCCC2)N(C3=CC(=CC=C3)F)C(=O)CN4C=CN=C4C
• InChI: InChI=1S/C27H31FN4O2/c1-19-9-6-7-14-24(19)26(27(34)30-22-11-4-3-5-12-22)32(23-13-8-10-21(28)17-23)25(33)18-31-16-15-29-20(31)2/h6-10,13-17,22,26H,3-5,11-12,18H2,1-2H3,(H,30,34)
• InChIKey: FNYGWXSATBUBER-UHFFFAOYSA-N
• PubChem CID: 56645356

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

Brain cancer [ICD-11: 2A00]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132H (c.395G>A)
• Sensitive Disease: FGFR-tacc positive glioblastoma [ICD-11: 2A00.01]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: TS676 cells; Brain; Homo sapiens (Human); CVCL_A5HX
• In Vitro Model: TS603 cells; Brain; Homo sapiens (Human); CVCL_A5HW
• In Vitro Model: TS516 cells; Brain; Homo sapiens (Human); CVCL_A5HY
• In Vivo Model: SCID mouse xenograft model; Mus musculus
• Experiment for Drug Resistance: Soft agar assay
• Mechanism Description: The missense mutation p.R132H (c.395G>A) in gene IDH1 cause the sensitivity of AGI-5198 by aberration of the drug's therapeutic target

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132C (c.394C>T)
• Sensitive Disease: Brain glioma [ICD-11: 2A00.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: TS676 cells; Brain; Homo sapiens (Human); CVCL_A5HX
• In Vitro Model: TS603 cells; Brain; Homo sapiens (Human); CVCL_A5HW
• In Vitro Model: TS516 cells; Brain; Homo sapiens (Human); CVCL_A5HY
• In Vivo Model: SCID mouse xenograft model; Mus musculus
• Experiment for Drug Resistance: Soft agar assay
• Mechanism Description: The missense mutation p.R132C (c.394C>T) in gene IDH1 cause the sensitivity of AGI-5198 by aberration of the drug's therapeutic target

Key Molecule: Oxalosuccinate decarboxylase (IDH1) [1]

• Molecule Alteration: Missense mutation; p.R132H (c.395G>A)
• Sensitive Disease: Brain glioma [ICD-11: 2A00.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: TS676 cells; Brain; Homo sapiens (Human); CVCL_A5HX
• In Vitro Model: TS603 cells; Brain; Homo sapiens (Human); CVCL_A5HW
• In Vitro Model: TS516 cells; Brain; Homo sapiens (Human); CVCL_A5HY
• In Vivo Model: SCID mouse xenograft model; Mus musculus
• Experiment for Drug Resistance: Soft agar assay
• Mechanism Description: The missense mutation p.R132H (c.395G>A) in gene IDH1 cause the sensitivity of AGI-5198 by aberration of the drug's therapeutic target

References

• Ref 1: An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cellsScience. 2013 May 3;340(6132):626-30. doi: 10.1126/science.1236062. Epub 2013 Apr 4.