| Drug General Information |
| Drug ID |
D0RT2C
|
| Former ID |
DIB007535
|
| Drug Name |
AZD9291
|
| Synonyms |
Tyrosine Kinase Inhibitor - Ns
|
| Drug Type |
Small molecular drug
|
| Indication |
Melanoma [ICD9: 172; ICD10:C43]
|
Phase 3 |
[1],
[2]
|
|---|
| Company |
Astrazeneca
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C28H33N7O2
|
| InChI |
InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)
|
| InChIKey |
DUYJMQONPNNFPI-UHFFFAOYSA-N
|
| PubChem Compound ID |
|
| PubChem Substance ID |
163477648, 182111940, 184525804, 184525822, 184525841, 184525860, 198967282, 210275341, 210280989, 223366052, 223370460, 223471425, 224657041, 226088106, 239637404, 242060364, 249735121, 249814472, 251910422, 252110297, 252151380, 252160935, 252214941, 252451374, 252551957, 252811262
|
| Drug Resistance Mutation (DRM) |
| DRM |
DRM Info
|
| Target and Pathway |
| Target(s) |
Epidermal growth factor receptor |
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 cancer
|
|
NetPath Pathway
|
IL4 Signaling Pathway
|
|
EGFR1 Signaling Pathway
|
|
PANTHER Pathway
|
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 events
|
|
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 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 interactions
|
| References |
| REF 1 | ClinicalTrials.gov (NCT02511106) AZD9291 Versus Placebo in Patients With Stage IB-IIIA Non-small Cell Lung Carcinoma, Following Complete Tumour Resection With or Without Adjuvant Chemotherapy. |
|---|
| REF 2 | (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: 7719). |
|---|
| REF 3 | AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. |
|---|
