Drug Information
Drug (ID: DG01619) and It's Reported Resistant Information
Name |
BAY1125976
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Synonyms |
BAY1125976; 1402608-02-9; BAY-1125976; UNII-ZL7A1UM87X; ZL7A1UM87X; 2-[4-(1-aminocyclobutyl)phenyl]-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide; Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-; 1402608-02-9 (free base); 2-(4-(1-aminocyclobutyl)phenyl)-3-phenylimidazo[1,2-b]pyridazine-6-carboxamide; 2-(4-(1-Aminocyclobutyl)phenyl)-3-phenylimidazo(1,2-b)pyridazine-6-carboxamide; Imidazo(1,2-b)pyridazine-6-carboxamide, 2-(4-(1-aminocyclobutyl)phenyl)-3-phenyl-; CHEMBL4751394; SCHEMBL12986078; US9604989, Example 5; GTPL10908; BDBM312517; BCP20659; CGC60802; EX-A3015; BAY112576; NSC793324; s8500; ZINC205604296; BAY-112576; CS-6212; NSC-793324; SB19771; BAY 1125976; Example 5 [WO2012136776A1]; AC-33646; HY-100018; BAY1125976;BAY 1125976; A921724
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Indication |
In total 2 Indication(s)
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Structure | |||||
Target | Proto-oncogene c-Met (MET) | MET_HUMAN | [1] | ||
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Formula |
4
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IsoSMILES |
C1CC(C1)(C2=CC=C(C=C2)C3=C(N4C(=N3)C=CC(=N4)C(=O)N)C5=CC=CC=C5)N
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InChI |
InChI=1S/C23H21N5O/c24-22(29)18-11-12-19-26-20(21(28(19)27-18)16-5-2-1-3-6-16)15-7-9-17(10-8-15)23(25)13-4-14-23/h1-3,5-12H,4,13-14,25H2,(H2,24,29)
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InChIKey |
JBGYKRAZYDNCNV-UHFFFAOYSA-N
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PubChem CID | |||||
TTD Drug ID |
Type(s) of Resistant Mechanism of This Drug
ADTT: Aberration of the Drug's Therapeutic Target
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Anal canal cancer [ICD-11: 2C00]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Aberration of the Drug's Therapeutic Target (ADTT) | ||||
Key Molecule: RAC-alpha serine/threonine-protein kinase (AKT1) | [1] | |||
Molecule Alteration | Missense mutation | p.E17K (c.49G>A) |
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Sensitive Disease | Anal canal cancer [ICD-11: 2C00.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | LNCaP cells | Prostate | Homo sapiens (Human) | CVCL_0395 |
MDA-MB-231 cells | Breast | Homo sapiens (Human) | CVCL_0062 | |
Hela cells | Cervix uteri | Homo sapiens (Human) | CVCL_0030 | |
NCI-H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
MDA-MB-453 cells | Breast | Homo sapiens (Human) | CVCL_0418 | |
MDA-MB-468 cells | Breast | Homo sapiens (Human) | CVCL_0419 | |
HCC70 cells | Breast | Homo sapiens (Human) | CVCL_1270 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
Caco-2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
MCF-7 cells | Breast | Homo sapiens (Human) | CVCL_0031 | |
ZR75-1 cells | Breast | Homo sapiens (Human) | CVCL_0588 | |
DU-145 cells | Prostate | Homo sapiens (Human) | CVCL_0105 | |
NCI-60 cells | N.A. | Homo sapiens (Human) | N.A. | |
EVSA-T cells | Ascites | Homo sapiens (Human) | CVCL_1207 | |
KU-19 cells | Blood | Bos taurus (Bovine) | CVCL_VN09 | |
T47D cells | Pleural effusion | Homo sapiens (Human) | CVCL_0553 | |
CAL-120 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1104 | |
BT-549 cells | Breast | Homo sapiens (Human) | CVCL_1092 | |
BT-474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
BT-20 cells | Mammary gland | Homo sapiens (Human) | CVCL_0178 | |
B16F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
In Vivo Model | Female NMRI (nu/nu) mouse xenograft model | Mus musculus | ||
Mechanism Description | The missense mutation p.E17K (c.49G>A) in gene AKT1 cause the sensitivity of BAY1125976 by aberration of the drug's therapeutic target |
Breast cancer [ICD-11: 2C60]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: RAC-alpha serine/threonine-protein kinase (AKT1) | [1] | |||
Molecule Alteration | Missense mutation | p.E17K (c.49G>A) |
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Sensitive Disease | Breast adenocarcinoma [ICD-11: 2C60.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | LNCaP cells | Prostate | Homo sapiens (Human) | CVCL_0395 |
MDA-MB-231 cells | Breast | Homo sapiens (Human) | CVCL_0062 | |
Hela cells | Cervix uteri | Homo sapiens (Human) | CVCL_0030 | |
NCI-H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
MDA-MB-453 cells | Breast | Homo sapiens (Human) | CVCL_0418 | |
MDA-MB-468 cells | Breast | Homo sapiens (Human) | CVCL_0419 | |
HCC70 cells | Breast | Homo sapiens (Human) | CVCL_1270 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
Caco-2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
MCF-7 cells | Breast | Homo sapiens (Human) | CVCL_0031 | |
ZR75-1 cells | Breast | Homo sapiens (Human) | CVCL_0588 | |
DU-145 cells | Prostate | Homo sapiens (Human) | CVCL_0105 | |
NCI-60 cells | N.A. | Homo sapiens (Human) | N.A. | |
EVSA-T cells | Ascites | Homo sapiens (Human) | CVCL_1207 | |
KU-19 cells | Blood | Bos taurus (Bovine) | CVCL_VN09 | |
T47D cells | Pleural effusion | Homo sapiens (Human) | CVCL_0553 | |
CAL-120 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1104 | |
BT-549 cells | Breast | Homo sapiens (Human) | CVCL_1092 | |
BT-474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
BT-20 cells | Mammary gland | Homo sapiens (Human) | CVCL_0178 | |
B16F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
In Vivo Model | Female NMRI (nu/nu) mouse xenograft model | Mus musculus | ||
Mechanism Description | The missense mutation p.E17K (c.49G>A) in gene AKT1 cause the sensitivity of BAY1125976 by unusual activation of pro-survival pathway | |||
Key Molecule: PI3-kinase alpha (PIK3CA) | [1] | |||
Molecule Alteration | Missense mutation | p.K111N (c.333G>C) |
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Sensitive Disease | Breast adenocarcinoma [ICD-11: 2C60.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | LNCaP cells | Prostate | Homo sapiens (Human) | CVCL_0395 |
MDA-MB-231 cells | Breast | Homo sapiens (Human) | CVCL_0062 | |
Hela cells | Cervix uteri | Homo sapiens (Human) | CVCL_0030 | |
NCI-H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
MDA-MB-453 cells | Breast | Homo sapiens (Human) | CVCL_0418 | |
MDA-MB-468 cells | Breast | Homo sapiens (Human) | CVCL_0419 | |
HCC70 cells | Breast | Homo sapiens (Human) | CVCL_1270 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
Caco-2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
MCF-7 cells | Breast | Homo sapiens (Human) | CVCL_0031 | |
ZR75-1 cells | Breast | Homo sapiens (Human) | CVCL_0588 | |
DU-145 cells | Prostate | Homo sapiens (Human) | CVCL_0105 | |
NCI-60 cells | N.A. | Homo sapiens (Human) | N.A. | |
EVSA-T cells | Ascites | Homo sapiens (Human) | CVCL_1207 | |
KU-19 cells | Blood | Bos taurus (Bovine) | CVCL_VN09 | |
T47D cells | Pleural effusion | Homo sapiens (Human) | CVCL_0553 | |
CAL-120 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1104 | |
BT-549 cells | Breast | Homo sapiens (Human) | CVCL_1092 | |
BT-474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
BT-20 cells | Mammary gland | Homo sapiens (Human) | CVCL_0178 | |
B16F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
In Vivo Model | Female NMRI (nu/nu) mouse xenograft model | Mus musculus | ||
Mechanism Description | The missense mutation p.K111N (c.333G>C) in gene PIK3CA cause the sensitivity of BAY1125976 by unusual activation of pro-survival pathway | |||
Key Molecule: PI3-kinase alpha (PIK3CA) | [1] | |||
Molecule Alteration | Missense mutation | p.P539R (c.1616C>G) |
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Sensitive Disease | Breast adenocarcinoma [ICD-11: 2C60.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | LNCaP cells | Prostate | Homo sapiens (Human) | CVCL_0395 |
MDA-MB-231 cells | Breast | Homo sapiens (Human) | CVCL_0062 | |
Hela cells | Cervix uteri | Homo sapiens (Human) | CVCL_0030 | |
NCI-H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
MDA-MB-453 cells | Breast | Homo sapiens (Human) | CVCL_0418 | |
MDA-MB-468 cells | Breast | Homo sapiens (Human) | CVCL_0419 | |
HCC70 cells | Breast | Homo sapiens (Human) | CVCL_1270 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
Caco-2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
MCF-7 cells | Breast | Homo sapiens (Human) | CVCL_0031 | |
ZR75-1 cells | Breast | Homo sapiens (Human) | CVCL_0588 | |
DU-145 cells | Prostate | Homo sapiens (Human) | CVCL_0105 | |
NCI-60 cells | N.A. | Homo sapiens (Human) | N.A. | |
EVSA-T cells | Ascites | Homo sapiens (Human) | CVCL_1207 | |
KU-19 cells | Blood | Bos taurus (Bovine) | CVCL_VN09 | |
T47D cells | Pleural effusion | Homo sapiens (Human) | CVCL_0553 | |
CAL-120 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1104 | |
BT-549 cells | Breast | Homo sapiens (Human) | CVCL_1092 | |
BT-474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
BT-20 cells | Mammary gland | Homo sapiens (Human) | CVCL_0178 | |
B16F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
In Vivo Model | Female NMRI (nu/nu) mouse xenograft model | Mus musculus | ||
Mechanism Description | The missense mutation p.P539R (c.1616C>G) in gene PIK3CA cause the sensitivity of BAY1125976 by unusual activation of pro-survival pathway | |||
Key Molecule: PI3-kinase alpha (PIK3CA) | [1] | |||
Molecule Alteration | Missense mutation | p.E545K (c.1633G>A) |
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Sensitive Disease | Breast adenocarcinoma [ICD-11: 2C60.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | LNCaP cells | Prostate | Homo sapiens (Human) | CVCL_0395 |
MDA-MB-231 cells | Breast | Homo sapiens (Human) | CVCL_0062 | |
Hela cells | Cervix uteri | Homo sapiens (Human) | CVCL_0030 | |
NCI-H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
MDA-MB-453 cells | Breast | Homo sapiens (Human) | CVCL_0418 | |
MDA-MB-468 cells | Breast | Homo sapiens (Human) | CVCL_0419 | |
HCC70 cells | Breast | Homo sapiens (Human) | CVCL_1270 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
Caco-2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
MCF-7 cells | Breast | Homo sapiens (Human) | CVCL_0031 | |
ZR75-1 cells | Breast | Homo sapiens (Human) | CVCL_0588 | |
DU-145 cells | Prostate | Homo sapiens (Human) | CVCL_0105 | |
NCI-60 cells | N.A. | Homo sapiens (Human) | N.A. | |
EVSA-T cells | Ascites | Homo sapiens (Human) | CVCL_1207 | |
KU-19 cells | Blood | Bos taurus (Bovine) | CVCL_VN09 | |
T47D cells | Pleural effusion | Homo sapiens (Human) | CVCL_0553 | |
CAL-120 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1104 | |
BT-549 cells | Breast | Homo sapiens (Human) | CVCL_1092 | |
BT-474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
BT-20 cells | Mammary gland | Homo sapiens (Human) | CVCL_0178 | |
B16F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
In Vivo Model | Female NMRI (nu/nu) mouse xenograft model | Mus musculus | ||
Mechanism Description | The missense mutation p.E545K (c.1633G>A) in gene PIK3CA cause the sensitivity of BAY1125976 by unusual activation of pro-survival pathway | |||
Key Molecule: PI3-kinase alpha (PIK3CA) | [1] | |||
Molecule Alteration | Missense mutation | p.H1047R (c.3140A>G) |
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Sensitive Disease | Breast adenocarcinoma [ICD-11: 2C60.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | LNCaP cells | Prostate | Homo sapiens (Human) | CVCL_0395 |
MDA-MB-231 cells | Breast | Homo sapiens (Human) | CVCL_0062 | |
Hela cells | Cervix uteri | Homo sapiens (Human) | CVCL_0030 | |
NCI-H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
MDA-MB-453 cells | Breast | Homo sapiens (Human) | CVCL_0418 | |
MDA-MB-468 cells | Breast | Homo sapiens (Human) | CVCL_0419 | |
HCC70 cells | Breast | Homo sapiens (Human) | CVCL_1270 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
Caco-2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
MCF-7 cells | Breast | Homo sapiens (Human) | CVCL_0031 | |
ZR75-1 cells | Breast | Homo sapiens (Human) | CVCL_0588 | |
DU-145 cells | Prostate | Homo sapiens (Human) | CVCL_0105 | |
NCI-60 cells | N.A. | Homo sapiens (Human) | N.A. | |
EVSA-T cells | Ascites | Homo sapiens (Human) | CVCL_1207 | |
KU-19 cells | Blood | Bos taurus (Bovine) | CVCL_VN09 | |
T47D cells | Pleural effusion | Homo sapiens (Human) | CVCL_0553 | |
CAL-120 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1104 | |
BT-549 cells | Breast | Homo sapiens (Human) | CVCL_1092 | |
BT-474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
BT-20 cells | Mammary gland | Homo sapiens (Human) | CVCL_0178 | |
B16F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
In Vivo Model | Female NMRI (nu/nu) mouse xenograft model | Mus musculus | ||
Mechanism Description | The missense mutation p.H1047R (c.3140A>G) in gene PIK3CA cause the sensitivity of BAY1125976 by unusual activation of pro-survival pathway | |||
Key Molecule: Phosphatase and tensin homolog (PTEN) | [1] | |||
Molecule Alteration | Missense mutation | p.L108R (c.323T>G) |
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Sensitive Disease | Breast adenocarcinoma [ICD-11: 2C60.1] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | LNCaP cells | Prostate | Homo sapiens (Human) | CVCL_0395 |
MDA-MB-231 cells | Breast | Homo sapiens (Human) | CVCL_0062 | |
Hela cells | Cervix uteri | Homo sapiens (Human) | CVCL_0030 | |
NCI-H460 cells | Lung | Homo sapiens (Human) | CVCL_0459 | |
MDA-MB-453 cells | Breast | Homo sapiens (Human) | CVCL_0418 | |
MDA-MB-468 cells | Breast | Homo sapiens (Human) | CVCL_0419 | |
HCC70 cells | Breast | Homo sapiens (Human) | CVCL_1270 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
Caco-2 cells | Colon | Homo sapiens (Human) | CVCL_0025 | |
MCF-7 cells | Breast | Homo sapiens (Human) | CVCL_0031 | |
ZR75-1 cells | Breast | Homo sapiens (Human) | CVCL_0588 | |
DU-145 cells | Prostate | Homo sapiens (Human) | CVCL_0105 | |
NCI-60 cells | N.A. | Homo sapiens (Human) | N.A. | |
EVSA-T cells | Ascites | Homo sapiens (Human) | CVCL_1207 | |
KU-19 cells | Blood | Bos taurus (Bovine) | CVCL_VN09 | |
T47D cells | Pleural effusion | Homo sapiens (Human) | CVCL_0553 | |
CAL-120 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1104 | |
BT-549 cells | Breast | Homo sapiens (Human) | CVCL_1092 | |
BT-474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | |
BT-20 cells | Mammary gland | Homo sapiens (Human) | CVCL_0178 | |
B16F10 cells | Skin | Mus musculus (Mouse) | CVCL_0159 | |
In Vivo Model | Female NMRI (nu/nu) mouse xenograft model | Mus musculus | ||
Mechanism Description | The missense mutation p.L108R (c.323T>G) in gene PTEN cause the sensitivity of BAY1125976 by unusual activation of pro-survival pathway |
References
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