Drug Information

Drug (ID: DG01627) and It's Reported Resistant Information

• Name: TAS-121
• Synonyms: UNII-Z36593C4RW; Z36593C4RW; SCHEMBL15220964; TAS-121; (S)-N-(4-amino-5-(quinolin-3-yl)-6,7,8,9-tetrahydropyrimido[5,4-b]indolizin-8-yl)acrylamide; 1451370-01-6; 2-Propenamide, N-((8S)-4-amino-6,7,8,9-tetrahydro-5-(3-quinolinyl)pyrimido(5,4-b)indolizin-8-yl)-; N-((8S)-4-Amino-6,7,8,9-tetrahydro-5-(3-quinolinyl)pyrimido(5,4-b)indolizin-8-yl)-2-propenamide
• Target: .; NOUNIPROTAC; [1]
• Formula: 3
• IsoSMILES: C=CC(=O)N[C@H]1CCC2=C(C3=C(N=CN=C3N2C1)N)C4=CC5=CC=CC=C5N=C4
• InChI: InChI=1S/C22H20N6O/c1-2-18(29)27-15-7-8-17-19(14-9-13-5-3-4-6-16(13)24-10-14)20-21(23)25-12-26-22(20)28(17)11-15/h2-6,9-10,12,15H,1,7-8,11H2,(H,27,29)(H2,23,25,26)/t15-/m0/s1
• InChIKey: POOPTPRMXSYFRV-HNNXBMFYSA-N
• PubChem CID: 71682991

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

Colorectal cancer [ICD-11: 2B91]

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.G719S (c.2155G>A)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: HEK293 cells; Kidney; Homo sapiens (Human); CVCL_0045
• In Vitro Model: SW48 cells; Colon; Homo sapiens (Human); CVCL_1724
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vivo Model: Male BALB/cA nude mouse xenograft model; Mus musculus
• Experiment for Drug Resistance: CellTiter-Glo assay; IC50 assay

Lung cancer [ICD-11: 2C25]

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.G719S (c.2155G>A)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: HEK293 cells; Kidney; Homo sapiens (Human); CVCL_0045
• In Vitro Model: SW48 cells; Colon; Homo sapiens (Human); CVCL_1724
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vivo Model: Male BALB/cA nude mouse xenograft model; Mus musculus
• Experiment for Drug Resistance: CellTiter-Glo assay; IC50 assay

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

• Molecule Alteration: Missense mutation; p.L858R (c.2573T>G)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: HEK293 cells; Kidney; Homo sapiens (Human); CVCL_0045
• In Vitro Model: SW48 cells; Colon; Homo sapiens (Human); CVCL_1724
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vivo Model: Male BALB/cA nude mouse xenograft model; Mus musculus
• Experiment for Drug Resistance: CellTiter-Glo assay; IC50 assay

References

• Ref 1: TAS-121, A Selective Mutant EGFR Inhibitor, Shows Activity Against Tumors Expressing Various EGFR Mutations Including T790M and Uncommon Mutations G719XMol Cancer Ther. 2019 May;18(5):920-928. doi: 10.1158/1535-7163.MCT-18-0645. Epub 2019 Mar 14.