Drug Information

Drug (ID: DG01635) and It's Reported Resistant Information
Name
BAY1217389
Synonyms
1554458-53-5; BAY1217389; Bay 1217389; BAY-1217389; UNII-M964LB1114; M964LB1114; Benzamide, N-cyclopropyl-4-[6-(2,3-difluoro-4-methoxyphenoxy)-8-[(3,3,3-trifluoropropyl)amino]imidazo[1,2-b]pyridazin-3-yl]-2-methyl-; N-cyclopropyl-4-[6-(2,3-difluoro-4-methoxyphenoxy)-8-(3,3,3-trifluoropropylamino)imidazo[1,2-b]pyridazin-3-yl]-2-methylbenzamide; N-Cyclopropyl-4-(6-(2,3-difluoro-4-methoxyphenoxy)-8-((3,3,3-trifluoropropyl)amino)imidazo[1,2-b]pyridazin-3-yl)-2-methylbenzamide; Benzamide, N-cyclopropyl-4-(6-(2,3-difluoro-4-methoxyphenoxy)-8-((3,3,3-trifluoropropyl)amino)imidazo(1,2-b)pyridazin-3-yl)-2-methyl-; N-cyclopropyl-4-[6-(2,3-difluoro-4-methoxyphenoxy)-8-[(3,3,3-trifluoropropyl)amino]imidazo[1,2-b]pyridazin-3-yl]-2-methylbenzamide; CHEMBL4456085; SCHEMBL15555839; EX-A948; BDBM258444; BCP17401; NSC787026; s8215; ZINC221039372; CCG-265387; CS-6182; NSC-787026; HY-12859; FT-0700219; US9512130, 2; J-690208; 1-(6-Isoquinolinyl)-3-[2-oxo-2-(1-pyrrolidinyl)ethyl]urea
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Structure
Target . NOUNIPROTAC [1]
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Formula
9
IsoSMILES
CC1=C(C=CC(=C1)C2=CN=C3N2N=C(C=C3NCCC(F)(F)F)OC4=C(C(=C(C=C4)OC)F)F)C(=O)NC5CC5
InChI
InChI=1S/C27H24F5N5O3/c1-14-11-15(3-6-17(14)26(38)35-16-4-5-16)19-13-34-25-18(33-10-9-27(30,31)32)12-22(36-37(19)25)40-21-8-7-20(39-2)23(28)24(21)29/h3,6-8,11-13,16,33H,4-5,9-10H2,1-2H3,(H,35,38)
InChIKey
WNEILUNVMHVMPH-UHFFFAOYSA-N
PubChem CID
78320750
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
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Colon cancer [ICD-11: 2B90]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Catenin beta-1 (CTNNB1) [1]
Molecule Alteration IF-deletion
p.S45delS (c.133_135delTCT)
 Molecule Info 
Sensitive Disease Colon cancer [ICD-11: 2B90.1]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HCT116 cells Colon Homo sapiens (Human) CVCL_0291
SW48 cells Colon Homo sapiens (Human) CVCL_1724
TOV-21G cells Ovary Homo sapiens (Human) CVCL_3613
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
TOV-112D cells Ovary Homo sapiens (Human) CVCL_3612
LS 174T cells Colon Homo sapiens (Human) CVCL_1384
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 BAY1217389 by unusual activation of pro-survival pathway.
Colorectal cancer [ICD-11: 2B91]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Catenin beta-1 (CTNNB1) [1]
Molecule Alteration Missense mutation
p.S45F (c.134C>T)
 Molecule Info 
Sensitive Disease Colorectal cancer [ICD-11: 2B91.1]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HCT116 cells Colon Homo sapiens (Human) CVCL_0291
SW48 cells Colon Homo sapiens (Human) CVCL_1724
TOV-21G cells Ovary Homo sapiens (Human) CVCL_3613
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
TOV-112D cells Ovary Homo sapiens (Human) CVCL_3612
LS 174T cells Colon Homo sapiens (Human) CVCL_1384
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.S45F (c.134C>T) in gene CTNNB1 cause the sensitivity of BAY1217389 by unusual activation of pro-survival pathway
Key Molecule: Catenin beta-1 (CTNNB1) [1]
Molecule Alteration Missense mutation
p.S33Y (c.98C>A)
 Molecule Info 
Sensitive Disease Colorectal cancer [ICD-11: 2B91.1]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HCT116 cells Colon Homo sapiens (Human) CVCL_0291
SW48 cells Colon Homo sapiens (Human) CVCL_1724
TOV-21G cells Ovary Homo sapiens (Human) CVCL_3613
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
TOV-112D cells Ovary Homo sapiens (Human) CVCL_3612
LS 174T cells Colon Homo sapiens (Human) CVCL_1384
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 BAY1217389 by unusual activation of pro-survival pathway
Lung cancer [ICD-11: 2C25]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Catenin beta-1 (CTNNB1) [1]
Molecule Alteration Missense mutation
p.T41A (c.121A>G)
 Molecule Info 
Sensitive Disease Lung adenocarcinoma [ICD-11: 2C25.0]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HCT116 cells Colon Homo sapiens (Human) CVCL_0291
SW48 cells Colon Homo sapiens (Human) CVCL_1724
TOV-21G cells Ovary Homo sapiens (Human) CVCL_3613
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
TOV-112D cells Ovary Homo sapiens (Human) CVCL_3612
LS 174T cells Colon Homo sapiens (Human) CVCL_1384
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 BAY1217389 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.

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