Drug Information

Drug (ID: DG01624) and It's Reported Resistant Information

• Name: BAY1161909
• Synonyms: Empesertib; 1443763-60-7; Mps1-IN-5; BAY 1161909; BAY-1161909; BAY1161909; UNII-02Y3Z2756M; 02Y3Z2756M; (2R)-2-(4-fluorophenyl)-N-[4-[2-(2-methoxy-4-methylsulfonylanilino)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]phenyl]propanamide; (-)-BAY-1161909; (2R)-2-(4-Fluorophenyl)-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)propanamide; (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide; Empesertib [INN]; Empesertib [WHO-DD]; GTPL9427; CHEMBL4303241; SCHEMBL15036597; BDBM329334; BCP23811; EX-A3543; BAY1161909;Mps1-IN-5; NSC787025; AKOS028109757; ZINC206769279; CS-4887; NSC-787025; US9663510, Example 01.01; NCGC00488781-01; AS-82506; BB177693; Benzeneacetamide, 4-fluoro-N-[4-[2-[[2-methoxy-4-(methylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a]; Benzeneacetamide, 4-fluoro-N-[4-[2-[[2-methoxy-4-(methylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a]pyridin-6-yl]phenyl]- -methyl-, ( R)-; HY-12858; D83662; A908652; BAY1161909; BAY-1161909; BAY 1161909;Mps1-IN-5; (2R)-2-(4-Fluorophenyl)-N-(4-(2-((4-(methanesulfonyl)-2-methoxyphenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)propanamide; (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]-amino}[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]propanamide; (2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(methylsulfonyl)phenyl]amino}[1,2,4]triazolo[1,5-alpha]pyridin-6-yl)phenyl]propanamide; (alphaR)-4-Fluoro-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)-alpha-methylbenzeneacetamide; Benzeneacetamide, 4-fluoro-N-(4-(2-((2-methoxy-4-(methylsulfonyl)phenyl)amino)(1,2,4)triazolo(1,5-a)pyridin-6-yl)phenyl)-alpha-methyl-, (alphaR)-
• Indication:
  In total 4 Indication(s)
  Gastrointestinal stromal tumour [ICD-11: 2B5B]; Phase 1; [1]
  Glioma [ICD-11: 2A00]; Phase 1; [1]
  Solid tumour/cancer [ICD-11: 2A00-2F9Z]; Phase 1; [1]
  Systemic mastocytosis [ICD-11: 2A21]; Phase 1; [1]
• Target: Platelet-derived growth factor receptor alpha (PDGFRA); PGFRA_HUMAN; [1]
• Target: Tyrosine-protein kinase Kit (KIT); KIT_HUMAN; [1]
• Formula: 8
• IsoSMILES: C[C@H](C1=CC=C(C=C1)F)C(=O)NC2=CC=C(C=C2)C3=CN4C(=NC(=N4)NC5=C(C=C(C=C5)S(=O)(=O)C)OC)C=C3
• InChI: InChI=1S/C29H26FN5O4S/c1-18(19-4-9-22(30)10-5-19)28(36)31-23-11-6-20(7-12-23)21-8-15-27-33-29(34-35(27)17-21)32-25-14-13-24(40(3,37)38)16-26(25)39-2/h4-18H,1-3H3,(H,31,36)(H,32,34)/t18-/m1/s1
• InChIKey: NRJKIOCCERLIDG-GOSISDBHSA-N
• PubChem CID: 71599640
• TTD Drug ID: D09AAK

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

Colon cancer [ICD-11: 2B90]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Catenin beta-1 (CTNNB1) [1]

• Molecule Alteration: IF-deletion; p.S45delS (c.133_135delTCT)
• Sensitive Disease: Colon cancer [ICD-11: 2B90.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: SW48 cells; Colon; Homo sapiens (Human); CVCL_1724
• In Vitro Model: TOV-21G cells; Ovary; Homo sapiens (Human); CVCL_3613
• In Vitro Model: HuTu80 cells; Small intestine; Homo sapiens (Human); CVCL_1301
• In Vitro Model: TOV-112D cells; Ovary; Homo sapiens (Human); CVCL_3612
• In Vitro Model: LS 174T cells; Colon; Homo sapiens (Human); CVCL_1384
• In Vitro Model: A427 cells; Lung; Homo sapiens (Human); CVCL_1055
• In Vivo Model: Mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Gene set analysis
• Experiment for Drug Resistance: Cell proliferation assay
• Mechanism Description: The if-deletion p.S45delS (c.133_135delTCT) in gene CTNNB1 cause the sensitivity of BAY1161909 by unusual activation of pro-survival pathway.

Colorectal cancer [ICD-11: 2B91]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Catenin beta-1 (CTNNB1) [1]

• Molecule Alteration: IF-deletion; p.S45delS (c.133_135delTCT)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: SW48 cells; Colon; Homo sapiens (Human); CVCL_1724
• In Vitro Model: TOV-21G cells; Ovary; Homo sapiens (Human); CVCL_3613
• In Vitro Model: HuTu80 cells; Small intestine; Homo sapiens (Human); CVCL_1301
• In Vitro Model: TOV-112D cells; Ovary; Homo sapiens (Human); CVCL_3612
• In Vitro Model: LS 174T cells; Colon; Homo sapiens (Human); CVCL_1384
• In Vitro Model: A427 cells; Lung; Homo sapiens (Human); CVCL_1055
• In Vivo Model: Mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Gene set analysis
• Experiment for Drug Resistance: Cell proliferation assay
• Mechanism Description: The if-deletion p.S45delS (c.133_135delTCT) in gene CTNNB1 cause the sensitivity of BAY1161909 by unusual activation of pro-survival pathway.

Key Molecule: Catenin beta-1 (CTNNB1) [1]

• Molecule Alteration: Missense mutation; p.S33Y (c.98C>A)
• Sensitive Disease: Colorectal cancer [ICD-11: 2B91.1]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: SW48 cells; Colon; Homo sapiens (Human); CVCL_1724
• In Vitro Model: TOV-21G cells; Ovary; Homo sapiens (Human); CVCL_3613
• In Vitro Model: HuTu80 cells; Small intestine; Homo sapiens (Human); CVCL_1301
• In Vitro Model: TOV-112D cells; Ovary; Homo sapiens (Human); CVCL_3612
• In Vitro Model: LS 174T cells; Colon; Homo sapiens (Human); CVCL_1384
• In Vitro Model: A427 cells; Lung; Homo sapiens (Human); CVCL_1055
• In Vivo Model: Mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Gene set analysis
• Experiment for Drug Resistance: Cell proliferation assay
• Mechanism Description: The missense mutation p.S33Y (c.98C>A) in gene CTNNB1 cause the sensitivity of BAY1161909 by unusual activation of pro-survival pathway

Lung cancer [ICD-11: 2C25]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Catenin beta-1 (CTNNB1) [1]

• Molecule Alteration: Missense mutation; p.T41A (c.121A>G)
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: HCT116 cells; Colon; Homo sapiens (Human); CVCL_0291
• In Vitro Model: SW48 cells; Colon; Homo sapiens (Human); CVCL_1724
• In Vitro Model: TOV-21G cells; Ovary; Homo sapiens (Human); CVCL_3613
• In Vitro Model: HuTu80 cells; Small intestine; Homo sapiens (Human); CVCL_1301
• In Vitro Model: TOV-112D cells; Ovary; Homo sapiens (Human); CVCL_3612
• In Vitro Model: LS 174T cells; Colon; Homo sapiens (Human); CVCL_1384
• In Vitro Model: A427 cells; Lung; Homo sapiens (Human); CVCL_1055
• In Vivo Model: Mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Gene set analysis
• Experiment for Drug Resistance: Cell proliferation assay
• Mechanism Description: The missense mutation p.T41A (c.121A>G) in gene CTNNB1 cause the sensitivity of BAY1161909 by unusual activation of pro-survival pathway

References

• Ref 1: TTK Inhibitors as a Targeted Therapy for CTNNB1 (Beta-catenin) Mutant CancersMol Cancer Ther. 2017 Nov;16(11):2609-2617. doi: 10.1158/1535-7163.MCT-17-0342. Epub 2017 Jul 27.