Drug Information

Drug (ID: DG01503) and It's Reported Resistant Information

• Name: TAE226
• Synonyms: 761437-28-9; NVP-TAE 226; NVP-TAE226; TAE226; 2-((5-Chloro-2-((2-methoxy-4-morpholinophenyl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide; TAE226 (NVP-TAE226); 2-({5-Chloro-2-[(2-Methoxy-4-Morpholin-4-Ylphenyl)amino]pyrimidin-4-Yl}amino)-N-Methylbenzamide; CHEMBL458997; TAE-226; CTx0152960; 1042432-58-5; 2-((5-CHLORO-2-((2-METHOXY-4-MORPHOLINOPHENYL)-AMINO)PYRIMIDIN-4-YL)AMINO)-N-METHYLBENZAMIDE; CTx-0152960;CTx 0152960; C23H25ClN6O3; 2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]-N-methylbenzamide; 2jkk; 2-[[5-chloro-2-[(2-methoxy-4-morpholin-4-ylphenyl)amino]pyrimidin-4-yl]amino]-N-methylbenzamide; BI9; Kinome_1212; NVP TAE226; NVPTAE 226; MLS006011059; SCHEMBL375524; GTPL9382; CHEBI:91452; DTXSID90433025; EX-A716; TAE 226; HMS3656L12; HMS3672E03; HMS3747C09; AOB87333; BCP06482; 1836AC; BDBM50334594; MFCD12031516; NSC787252; s2820; ZINC20148986; AKOS016004135; CCG-269438; CS-0594; DB07460; NSC-787252; SB19397; 2-({5-Chloro-2-[2-methoxy-4-(morpholin-4-yl)anilino]pyrimidin-4-yl}amino)-N-methylbenzamide; NCGC00346931-01; NCGC00346931-05; 2-[5-chloro-2-(2-methoxy-4-morpholin-4-yl-phenylamino)-pyrimidin-4-ylamino]-N-methyl-benzamide; AC-27408; AS-56281; HY-13203; SMR004702851; FT-0700360; SW219314-1; NVP-TAE 226,CAS:761437-28-9; A865545; J-690348; Q27096680; 2-({5-Chloro-2-[2-methoxy-4-(4-morpholinyl)anilino]-4-pyrimidinyl}amino)-N-methylbenzamide; 2-(5-chloro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)-N-methylbenzamide; 2-[5-chloro-2-[2-methoxy-4-(4-morpholinyl)phenylamino]pyrimidin-4-ylamino]-N-methylbenzamide
• Target: .; NOUNIPROTAC; [1]
• Formula: 7
• IsoSMILES: CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCOCC4)OC
• InChI: InChI=1S/C23H25ClN6O3/c1-25-22(31)16-5-3-4-6-18(16)27-21-17(24)14-26-23(29-21)28-19-8-7-15(13-20(19)32-2)30-9-11-33-12-10-30/h3-8,13-14H,9-12H2,1-2H3,(H,25,31)(H2,26,27,28,29)
• InChIKey: UYJNQQDJUOUFQJ-UHFFFAOYSA-N
• PubChem CID: 9934347

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

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

Unusual Activation of Pro-survival Pathway (UAPP)

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: Revealed Based on the Cell Line Data
• In Vitro Model: NCI-H2228 cells; Lung; Homo sapiens (Human); CVCL_1543
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: NCI-H838 cells; Lung; Homo sapiens (Human); CVCL_1594
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HCC4006 cells; Lung; Homo sapiens (Human); CVCL_1269
• In Vitro Model: NCI-H1395 cells; Lung; Homo sapiens (Human); CVCL_1467
• In Vitro Model: SkBR3 cells; Breast; Homo sapiens (Human); CVCL_0033
• In Vitro Model: HEK293T cells; Kidney; Homo sapiens (Human); CVCL_0063
• In Vitro Model: NCI-H820 cells; Lymph node; Homo sapiens (Human); CVCL_1592
• In Vitro Model: NCI-H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vitro Model: NCI-H1993 cells; Lymph node; Homo sapiens (Human); CVCL_1512
• In Vitro Model: NCI-H1819 cells; Lymph node; Homo sapiens (Human); CVCL_1497
• In Vitro Model: NCI-H1666 cells; Pleural effusion; Homo sapiens (Human); CVCL_1485
• In Vitro Model: NCI-H1648 cells; Lymph node; Homo sapiens (Human); CVCL_1482
• In Vitro Model: NCI-H1299 cells; Lymph node; Homo sapiens (Human); CVCL_0060
• In Vitro Model: MKN45 cells; Liver; Homo sapiens (Human); CVCL_0434
• In Vivo Model: BALB/c-nu/nu female nude mouse PC9 xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: CellTiter-96 AQueous One assay

Lung cancer [ICD-11: 2C25]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]

• Molecule Alteration: Missense mutation; p.G466V (c.1397G>T)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: NCI-H2228 cells; Lung; Homo sapiens (Human); CVCL_1543
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: NCI-H838 cells; Lung; Homo sapiens (Human); CVCL_1594
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HCC4006 cells; Lung; Homo sapiens (Human); CVCL_1269
• In Vitro Model: NCI-H1395 cells; Lung; Homo sapiens (Human); CVCL_1467
• In Vitro Model: SkBR3 cells; Breast; Homo sapiens (Human); CVCL_0033
• In Vitro Model: HEK293T cells; Kidney; Homo sapiens (Human); CVCL_0063
• In Vitro Model: NCI-H820 cells; Lymph node; Homo sapiens (Human); CVCL_1592
• In Vitro Model: NCI-H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vitro Model: NCI-H1993 cells; Lymph node; Homo sapiens (Human); CVCL_1512
• In Vitro Model: NCI-H1819 cells; Lymph node; Homo sapiens (Human); CVCL_1497
• In Vitro Model: NCI-H1666 cells; Pleural effusion; Homo sapiens (Human); CVCL_1485
• In Vitro Model: NCI-H1648 cells; Lymph node; Homo sapiens (Human); CVCL_1482
• In Vitro Model: NCI-H1299 cells; Lymph node; Homo sapiens (Human); CVCL_0060
• In Vitro Model: MKN45 cells; Liver; Homo sapiens (Human); CVCL_0434
• In Vivo Model: BALB/c-nu/nu female nude mouse PC9 xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: CellTiter-96 AQueous One assay

Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]

• Molecule Alteration: Missense mutation; p.G469A (c.1406G>C)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: NCI-H2228 cells; Lung; Homo sapiens (Human); CVCL_1543
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: NCI-H838 cells; Lung; Homo sapiens (Human); CVCL_1594
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HCC4006 cells; Lung; Homo sapiens (Human); CVCL_1269
• In Vitro Model: NCI-H1395 cells; Lung; Homo sapiens (Human); CVCL_1467
• In Vitro Model: SkBR3 cells; Breast; Homo sapiens (Human); CVCL_0033
• In Vitro Model: HEK293T cells; Kidney; Homo sapiens (Human); CVCL_0063
• In Vitro Model: NCI-H820 cells; Lymph node; Homo sapiens (Human); CVCL_1592
• In Vitro Model: NCI-H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vitro Model: NCI-H1993 cells; Lymph node; Homo sapiens (Human); CVCL_1512
• In Vitro Model: NCI-H1819 cells; Lymph node; Homo sapiens (Human); CVCL_1497
• In Vitro Model: NCI-H1666 cells; Pleural effusion; Homo sapiens (Human); CVCL_1485
• In Vitro Model: NCI-H1648 cells; Lymph node; Homo sapiens (Human); CVCL_1482
• In Vitro Model: NCI-H1299 cells; Lymph node; Homo sapiens (Human); CVCL_0060
• In Vitro Model: MKN45 cells; Liver; Homo sapiens (Human); CVCL_0434
• In Vivo Model: BALB/c-nu/nu female nude mouse PC9 xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: CellTiter-96 AQueous One 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: NCI-H2228 cells; Lung; Homo sapiens (Human); CVCL_1543
• In Vitro Model: HCC827 cells; Lung; Homo sapiens (Human); CVCL_2063
• In Vitro Model: NCI-H838 cells; Lung; Homo sapiens (Human); CVCL_1594
• In Vitro Model: NCI-H1975 cells; Lung; Homo sapiens (Human); CVCL_1511
• In Vitro Model: HCC4006 cells; Lung; Homo sapiens (Human); CVCL_1269
• In Vitro Model: NCI-H1395 cells; Lung; Homo sapiens (Human); CVCL_1467
• In Vitro Model: SkBR3 cells; Breast; Homo sapiens (Human); CVCL_0033
• In Vitro Model: HEK293T cells; Kidney; Homo sapiens (Human); CVCL_0063
• In Vitro Model: NCI-H820 cells; Lymph node; Homo sapiens (Human); CVCL_1592
• In Vitro Model: NCI-H3255 cells; Lung; Homo sapiens (Human); CVCL_6831
• In Vitro Model: NCI-H1993 cells; Lymph node; Homo sapiens (Human); CVCL_1512
• In Vitro Model: NCI-H1819 cells; Lymph node; Homo sapiens (Human); CVCL_1497
• In Vitro Model: NCI-H1666 cells; Pleural effusion; Homo sapiens (Human); CVCL_1485
• In Vitro Model: NCI-H1648 cells; Lymph node; Homo sapiens (Human); CVCL_1482
• In Vitro Model: NCI-H1299 cells; Lymph node; Homo sapiens (Human); CVCL_0060
• In Vitro Model: MKN45 cells; Liver; Homo sapiens (Human); CVCL_0434
• In Vivo Model: BALB/c-nu/nu female nude mouse PC9 xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: CellTiter-96 AQueous One assay

References

• Ref 1: TAE226, a Bis-Anilino Pyrimidine Compound, Inhibits the EGFR-Mutant Kinase Including T790M Mutant to Show Anti-Tumor Effect on EGFR-Mutant Non-Small Cell Lung Cancer CellsPLoS One. 2015 Jun 19;10(6):e0129838. doi: 10.1371/journal.pone.0129838. eCollection 2015.