| Drug General Information |
| Drug ID |
D0A9OV
|
| Former ID |
DCL000347
|
| Drug Name |
TAK165
|
| Synonyms |
Mubritinib; TAK 165; Mubritinib (USAN/INN); 4-[[4-[4-(triazol-1-yl)butyl]phenoxy]methyl]-2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,3-oxazole
|
| Drug Type |
Small molecular drug
|
| Indication |
Cancer [ICD9: 140-229; ICD10:C00-C96]
|
Discontinued in Phase 1 |
[1],
[2]
|
|---|
| Therapeutic Class |
Anticancer Agents
|
| Company |
Takeda Pharmaceuticals
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C25H23F3N4O2
|
| InChI |
InChI=1S/C25H23F3N4O2/c26-25(27,28)21-9-4-20(5-10-21)8-13-24-30-22(18-34-24)17-33-23-11-6-19(7-12-23)3-1-2-15-32-16-14-29-31-32/h4-14,16,18H,1-3,15,17H2/b13-8+
|
| InChIKey |
ZTFBIUXIQYRUNT-MDWZMJQESA-N
|
| CAS Number |
CAS 366017-09-6
|
| PubChem Compound ID |
|
| PubChem Substance ID |
11969389, 14760763, 17398009, 43037052, 50490680, 57369821, 92721420, 99299526, 114571134, 123122738, 124360689, 124757654, 125164458, 126619164, 126661686, 131312231, 135178532, 135698690, 136348757, 136349478, 136367609, 137124306, 143157306, 144115322, 152057420, 152344431, 160682577, 162011934, 162037824, 162202684, 178102633, 179150389, 179322939, 186009055, 198947389, 204359629, 223396725, 223668772, 223704690, 223786982, 226472299, 241073514, 252157389, 252160688, 252215852, 252451421, 252543383
|
| Target and Pathway |
| Target(s) |
Epidermal growth factor receptor |
Target Info |
Inhibitor |
[3]
|
|---|
| Receptor protein-tyrosine kinase erbB-2 |
Target Info |
Inhibitor |
[3]
|
|
KEGG Pathway
|
MAPK signaling pathway
|
|
ErbB signaling pathway
|
|
Ras signaling pathway
|
|
Rap1 signaling pathway
|
|
Calcium signaling pathway
|
|
Cytokine-cytokine receptor interaction
|
|
HIF-1 signaling pathway
|
|
FoxO signaling pathway
|
|
Endocytosis
|
|
PI3K-Akt signaling pathway
|
|
Dorso-ventral axis formation
|
|
Focal adhesion
|
|
Adherens junction
|
|
Gap junction
|
|
Regulation of actin cytoskeleton
|
|
GnRH signaling pathway
|
|
Estrogen signaling pathway
|
|
Oxytocin signaling pathway
|
|
Epithelial cell signaling in Helicobacter pylori infection
|
|
Hepatitis C
|
|
Pathways in cancer
|
|
Proteoglycans in cancer
|
|
MicroRNAs in cancer
|
|
Pancreatic cancer
|
|
Endometrial cancer
|
|
Glioma
|
|
Prostate cancer
|
|
Melanoma
|
|
Bladder cancer
|
|
Non-small cell lung cancer
|
|
Central carbon metabolism in cancer
|
|
Choline metabolism in cancerhsa04012:ErbB signaling pathway
|
|
NetPath Pathway
|
IL4 Signaling Pathway
|
|
EGFR1 Signaling PathwayNetPath_11:TCR Signaling Pathway
|
|
PANTHER Pathway
|
Cadherin signaling pathway
|
|
EGF receptor signaling pathwayP00012:Cadherin signaling pathway
|
|
EGF receptor signaling pathway
|
|
Pathway Interaction Database
|
LPA receptor mediated events
|
|
Signaling events mediated by PTP1B
|
|
Arf6 signaling events
|
|
Signaling events mediated by TCPTP
|
|
Thromboxane A2 receptor signaling
|
|
SHP2 signaling
|
|
Regulation of Telomerase
|
|
EGF receptor (ErbB1) signaling pathway
|
|
EGFR-dependent Endothelin signaling events
|
|
Posttranslational regulation of adherens junction stability and dissassembly
|
|
Direct p53 effectors
|
|
ErbB1 downstream signaling
|
|
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
|
|
E-cadherin signaling in keratinocytes
|
|
ErbB receptor signaling network
|
|
Internalization of ErbB1
|
|
Stabilization and expansion of the E-cadherin adherens junction
|
|
a6b1 and a6b4 Integrin signaling
|
|
Syndecan-3-mediated signaling eventserbb4_pathway:ErbB4 signaling events
|
|
ErbB2/ErbB3 signaling events
|
|
Validated targets of C-MYC transcriptional repression
|
|
PathWhiz Pathway
|
Phosphatidylinositol Phosphate Metabolism
|
|
Reactome
|
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
|
|
SHC1 events in ERBB2 signaling
|
|
PLCG1 events in ERBB2 signaling
|
|
PIP3 activates AKT signaling
|
|
GRB2 events in EGFR signaling
|
|
GAB1 signalosome
|
|
SHC1 events in EGFR signaling
|
|
EGFR downregulation
|
|
GRB2 events in ERBB2 signaling
|
|
PI3K events in ERBB2 signaling
|
|
EGFR Transactivation by Gastrin
|
|
Constitutive Signaling by Aberrant PI3K in Cancer
|
|
Constitutive Signaling by EGFRvIII
|
|
RAF/MAP kinase cascadeR-HSA-1250196:SHC1 events in ERBB2 signaling
|
|
Sema4D induced cell migration and growth-cone collapse
|
|
RAF/MAP kinase cascade
|
|
WikiPathways
|
ErbB Signaling Pathway
|
|
Regulation of Actin Cytoskeleton
|
|
EGF/EGFR Signaling Pathway
|
|
MAPK Signaling Pathway
|
|
Focal Adhesion
|
|
Aryl Hydrocarbon Receptor Pathway
|
|
Extracellular vesicle-mediated signaling in recipient cells
|
|
TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer
|
|
Hair Follicle Development: Cytodifferentiation (Part 3 of 3)
|
|
Bladder Cancer
|
|
Hair Follicle Development: Induction (Part 1 of 3)
|
|
Signaling by ERBB4
|
|
Signaling by ERBB2
|
|
Gastrin-CREB signalling pathway via PKC and MAPK
|
|
PIP3 activates AKT signaling
|
|
Nanoparticle-mediated activation of receptor signaling
|
|
Aryl Hydrocarbon Receptor
|
|
Spinal Cord Injury
|
|
Integrated Pancreatic Cancer Pathway
|
|
Gastric cancer network 2
|
|
AGE/RAGE pathway
|
|
Signaling Pathways in Glioblastoma
|
|
Arylhydrocarbon receptor (AhR) signaling pathway
|
|
miR-targeted genes in muscle cell - TarBase
|
|
miR-targeted genes in lymphocytes - TarBase
|
|
miR-targeted genes in epithelium - TarBase
|
|
Integrated Breast Cancer Pathway
|
|
Signaling by EGFR
|
|
L1CAM interactionsWP710:DNA Damage Response (only ATM dependent)
|
|
Leptin signaling pathway
|
|
Semaphorin interactions
|
| References |
| REF 1 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6011). |
|---|
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019257) |
|---|
| REF 3 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. |
|---|
