| Drug General Information |
| Drug ID |
D0YB3W
|
| Former ID |
DCL000086
|
| Drug Name |
CI-1033
|
| Synonyms |
Canertinib; Canertinib HCl; Canertinib dihydrochloride; Canertinib dihydrochloride [USAN]; CI1033; PD 183805; Canertinib dihydrochloride (USAN); PD-0183805; PD-183805; Canertinib, PD-183805, CI1033, PD183805; N-[4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide dihydrochloride; N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide dihydrochloride; N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide; N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide dihydrochloride; N-(4-(3-chloro-4-fluorophenyl)amino)-7-(3-morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide dihydrochloride; N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide; N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-(morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide; 2-Propenamide, N-(4-((3-chloro-4-fluorophenyl) amino)-7-(3-(4-morpholinyl) propoxy)-6-quinazolinyl)-, dihydrochloride; 2-Propenamide, N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-(4-morpholinyl)propoxy)-6-quinazolinyl)-, dihydrochloride
|
| Drug Type |
Small molecular drug
|
| Indication |
Lymphoma [ICD9: 202.8, 208.9; ICD10:C81-C86]
|
Phase 2 |
[1],
[2]
|
|---|
| Therapeutic Class |
Anticancer Agents
|
| Company |
Pfizer
|
| Structure |
|
Download
2D MOL
3D MOL
|
| Formula |
C24H25ClFN5O3
|
| InChI |
InChI=1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)
|
| InChIKey |
OMZCMEYTWSXEPZ-UHFFFAOYSA-N
|
| CAS Number |
CAS 289499-45-2
|
| PubChem Compound ID |
|
| PubChem Substance ID |
8034429, 10252913, 14883693, 46232231, 50100094, 50917991, 90342405, 99299163, 99432370, 103202250, 109693018, 111978347, 113435040, 123121573, 124756938, 124894124, 125163745, 125346553, 126645791, 126671639, 126731255, 127318548, 127318549, 127318550, 127318551, 127318552, 127318553, 128832430, 131465108, 134964336, 135187325, 135685374, 135685375, 135685393, 135727440, 136368009, 137059481, 137237688, 141965894, 143497675, 144115783, 144115784, 144115827, 144206912, 152234940, 152258193, 152344143, 160647029, 162011526, 162037387
|
| Target and Pathway |
| Target(s) |
Receptor protein-tyrosine kinase erbB-2 |
Target Info |
Inhibitor |
[3]
|
|---|
| Receptor protein-tyrosine kinase erbB-4 |
Target Info |
Inhibitor |
[4],
[3]
|
| Epidermal growth factor receptor |
Target Info |
Inhibitor |
[3]
|
| RAC serine/threonine-protein kinase |
Target Info |
Inhibitor |
[3]
|
|
KEGG Pathway
|
ErbB signaling pathway
|
|
Calcium signaling pathway
|
|
HIF-1 signaling pathway
|
|
Focal adhesion
|
|
Adherens junction
|
|
Pathways in cancer
|
|
Proteoglycans in cancer
|
|
MicroRNAs in cancer
|
|
Pancreatic cancer
|
|
Endometrial cancer
|
|
Prostate cancer
|
|
Bladder cancer
|
|
Non-small cell lung cancer
|
|
Central carbon metabolism in cancerhsa04012:ErbB signaling pathway
|
|
Endocytosis
|
|
Proteoglycans in cancerhsa04010:MAPK signaling pathway
|
|
Ras signaling pathway
|
|
Rap1 signaling pathway
|
|
Cytokine-cytokine receptor interaction
|
|
FoxO signaling pathway
|
|
PI3K-Akt signaling pathway
|
|
Dorso-ventral axis formation
|
|
Gap junction
|
|
Regulation of actin cytoskeleton
|
|
GnRH signaling pathway
|
|
Estrogen signaling pathway
|
|
Oxytocin signaling pathway
|
|
Epithelial cell signaling in Helicobacter pylori infection
|
|
Hepatitis C
|
|
Glioma
|
|
Melanoma
|
|
Central carbon metabolism in cancer
|
|
Choline metabolism in cancerhsa04010:MAPK signaling pathway
|
|
cGMP-PKG signaling pathway
|
|
cAMP signaling pathway
|
|
Chemokine signaling pathway
|
|
Sphingolipid signaling pathway
|
|
mTOR signaling pathway
|
|
AMPK signaling pathway
|
|
Apoptosis
|
|
Adrenergic signaling in cardiomyocytes
|
|
VEGF signaling pathway
|
|
Osteoclast differentiation
|
|
Tight junction
|
|
Signaling pathways regulating pluripotency of stem cells
|
|
Platelet activation
|
|
Toll-like receptor signaling pathway
|
|
Jak-STAT signaling pathway
|
|
T cell receptor signaling pathway
|
|
B cell receptor signaling pathway
|
|
Fc epsilon RI signaling pathway
|
|
Fc gamma R-mediated phagocytosis
|
|
TNF signaling pathway
|
|
Neurotrophin signaling pathway
|
|
Cholinergic synapse
|
|
Dopaminergic synapse
|
|
Insulin signaling pathway
|
|
Progesterone-mediated oocyte maturation
|
|
Prolactin signaling pathway
|
|
Thyroid hormone signaling pathway
|
|
Adipocytokine signaling pathway
|
|
Glucagon signaling pathway
|
|
Regulation of lipolysis in adipocytes
|
|
Non-alcoholic fatty liver disease (NAFLD)
|
|
Carbohydrate digestion and absorption
|
|
Chagas disease (American trypanosomiasis)
|
|
Toxoplasmosis
|
|
Tuberculosis
|
|
Hepatitis B
|
|
Measles
|
|
Influenza A
|
|
HTLV-I infection
|
|
Epstein-Barr virus infection
|
|
Colorectal cancer
|
|
Renal cell carcinoma
|
|
Chronic myeloid leukemia
|
|
Acute myeloid leukemia
|
|
Small cell lung cancer
|
|
Choline metabolism in cancer
|
|
NetPath Pathway
|
TCR Signaling PathwayNetPath_16:IL4 Signaling Pathway
|
|
EGFR1 Signaling PathwayNetPath_23:TSH Signaling Pathway
|
|
PANTHER Pathway
|
Cadherin signaling pathway
|
|
EGF receptor signaling pathwayP00004:Alzheimer disease-presenilin pathway
|
|
EGF receptor signaling pathwayP00012:Cadherin signaling pathway
|
|
EGF receptor signaling pathwayP00005:Angiogenesis
|
|
Apoptosis signaling pathway
|
|
EGF receptor signaling pathway
|
|
Endothelin signaling pathway
|
|
FGF signaling pathway
|
|
Huntington disease
|
|
Hypoxia response via HIF activation
|
|
Inflammation mediated by chemokine and cytokine signaling pathway
|
|
Insulin/IGF pathway-protein kinase B signaling cascade
|
|
Interleukin signaling pathway
|
|
PI3 kinase pathway
|
|
T cell activation
|
|
VEGF signaling pathway
|
|
p53 pathway
|
|
Ras Pathway
|
|
p53 pathway by glucose deprivation
|
|
p53 pathway feedback loops 2
|
|
CCKR signaling map ST
|
|
Pathway Interaction Database
|
ErbB4 signaling events
|
|
ErbB2/ErbB3 signaling events
|
|
ErbB receptor signaling network
|
|
a6b1 and a6b4 Integrin signaling
|
|
Validated targets of C-MYC transcriptional repressionlysophospholipid_pathway: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
|
|
Internalization of ErbB1
|
|
Stabilization and expansion of the E-cadherin adherens junction
|
|
Syndecan-3-mediated signaling eventssmad2_3nuclearpathway:Regulation of nuclear SMAD2/3 signaling
|
|
Fc-epsilon receptor I signaling in mast cells
|
|
Endothelins
|
|
BCR signaling pathway
|
|
LPA receptor mediated events
|
|
Insulin Pathway
|
|
IL4-mediated signaling events
|
|
TCR signaling in naï
|
|
Plasma membrane estrogen receptor signaling
|
|
CD40/CD40L signaling
|
|
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
|
|
S1P3 pathway
|
|
Coregulation of Androgen receptor activity
|
|
Reelin signaling pathway
|
|
Integrin-linked kinase signaling
|
|
TCR signaling in naï
|
|
Angiopoietin receptor Tie2-mediated signaling
|
|
FAS (CD95) signaling pathway
|
|
FOXA2 and FOXA3 transcription factor networks
|
|
Glucocorticoid receptor regulatory network
|
|
mTOR signaling pathway
|
|
CXCR4-mediated signaling events
|
|
IGF1 pathway
|
|
FoxO family signaling
|
|
IL2 signaling events mediated by PI3K
|
|
Ceramide signaling pathway
|
|
p75(NTR)-mediated signaling
|
|
E-cadherin signaling in the nascent adherens junction
|
|
amb2 Integrin signaling
|
|
Integrins in angiogenesis
|
|
IFN-gamma pathway
|
|
IL6-mediated signaling events
|
|
Nephrin/Neph1 signaling in the kidney podocyte
|
|
Retinoic acid receptors-mediated signaling
|
|
IL8- and CXCR2-mediated signaling events
|
|
Signaling events mediated by the Hedgehog family
|
|
Nongenotropic Androgen signaling
|
|
Hedgehog signaling events mediated by Gli proteins
|
|
Caspase Cascade in Apoptosis
|
|
CXCR3-mediated signaling events
|
|
VEGFR1 specific signals
|
|
Signaling events mediated by Stem cell factor receptor (c-Kit)
|
|
Signaling events mediated by VEGFR1 and VEGFR2
|
|
Aurora A signaling
|
|
Insulin-mediated glucose transport
|
|
Class I PI3K signaling events mediated by Akt
|
|
IL8- and CXCR1-mediated signaling events
|
|
HIF-1-alpha transcription factor network
|
|
p53 pathway
|
|
Trk receptor signaling mediated by PI3K and PLC-gamma
|
|
VEGFR3 signaling in lymphatic endothelium
|
|
FGF signaling pathway
|
|
PathWhiz Pathway
|
Phosphatidylinositol Phosphate MetabolismPW000445:Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
|
|
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
|
|
Fc Epsilon Receptor I Signaling in Mast Cells
|
|
Insulin Signalling
|
|
Leucine Stimulation on Insulin Signaling
|
|
Reactome
|
SHC1 events in ERBB2 signaling
|
|
PLCG1 events in ERBB2 signaling
|
|
PIP3 activates AKT signaling
|
|
GRB2 events in ERBB2 signaling
|
|
PI3K events in ERBB2 signaling
|
|
Constitutive Signaling by Aberrant PI3K in Cancer
|
|
Sema4D induced cell migration and growth-cone collapse
|
|
RAF/MAP kinase cascadeR-HSA-1236382:Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
|
|
GRB2 events in EGFR signaling
|
|
GAB1 signalosome
|
|
SHC1 events in EGFR signaling
|
|
EGFR downregulation
|
|
EGFR Transactivation by Gastrin
|
|
Constitutive Signaling by EGFRvIII
|
|
RAF/MAP kinase cascadeR-HSA-111447:Activation of BAD and translocation to mitochondria
|
|
GPVI-mediated activation cascade
|
|
Translocation of GLUT4 to the plasma membrane
|
|
Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation
|
|
AKT phosphorylates targets in the cytosol
|
|
AKT phosphorylates targets in the nucleus
|
|
Negative regulation of the PI3K/AKT network
|
|
eNOS activation
|
|
AKT-mediated inactivation of FOXO1A
|
|
Integrin alphaIIb beta3 signaling
|
|
Deactivation of the beta-catenin transactivating complex
|
|
CD28 dependent PI3K/Akt signaling
|
|
CTLA4 inhibitory signaling
|
|
G beta:gamma signalling through PI3Kgamma
|
|
KSRP (KHSRP) binds and destabilizes mRNA
|
|
VEGFR2 mediated vascular permeability
|
|
TP53 Regulates Metabolic Genes
|
|
Constitutive Signaling by AKT1 E17K in Cancer
|
|
WikiPathways
|
DNA Damage Response (only ATM dependent)
|
|
ErbB Signaling Pathway
|
|
EGF/EGFR Signaling Pathway
|
|
Focal Adhesion
|
|
Extracellular vesicle-mediated signaling in recipient cells
|
|
Bladder Cancer
|
|
Signaling by ERBB2
|
|
Integrated Pancreatic Cancer Pathway
|
|
Signaling Pathways in Glioblastoma
|
|
Leptin signaling pathway
|
|
miR-targeted genes in muscle cell - TarBase
|
|
Semaphorin interactionsWP673:ErbB Signaling Pathway
|
|
EV release from cardiac cells and their functional effectsWP673:ErbB Signaling Pathway
|
|
Regulation of Actin Cytoskeleton
|
|
MAPK Signaling Pathway
|
|
Aryl Hydrocarbon Receptor Pathway
|
|
TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer
|
|
Hair Follicle Development: Cytodifferentiation (Part 3 of 3)
|
|
Hair Follicle Development: Induction (Part 1 of 3)
|
|
Signaling by ERBB4
|
|
Gastrin-CREB signalling pathway via PKC and MAPK
|
|
PIP3 activates AKT signaling
|
|
Nanoparticle-mediated activation of receptor signaling
|
|
Aryl Hydrocarbon Receptor
|
|
Spinal Cord Injury
|
|
Gastric cancer network 2
|
|
AGE/RAGE pathway
|
|
Arylhydrocarbon receptor (AhR) signaling pathway
|
|
miR-targeted genes in lymphocytes - TarBase
|
|
miR-targeted genes in epithelium - TarBase
|
|
Integrated Breast Cancer Pathway
|
|
Signaling by EGFR
|
|
L1CAM interactionsWP75:Toll-like receptor signaling pathway
|
|
TCR Signaling Pathway
|
|
Notch Signaling Pathway
|
|
EPO Receptor Signaling
|
|
IL-2 Signaling Pathway
|
|
Insulin Signaling
|
|
Endochondral Ossification
|
|
IL-4 Signaling Pathway
|
|
TGF beta Signaling Pathway
|
|
IL-6 signaling pathway
|
|
Wnt Signaling Pathway Netpath
|
|
Copper homeostasis
|
|
Apoptosis-related network due to altered Notch3 in ovarian cancer
|
|
IL-3 Signaling Pathway
|
|
Cardiac Hypertrophic Response
|
|
Translocation of GLUT4 to the Plasma Membrane
|
|
Regulation of mRNA Stability by Proteins that Bind AU-rich Elements
|
|
Signal Transduction of S1P Receptor
|
|
T-Cell Receptor and Co-stimulatory Signaling
|
|
Primary Focal Segmental Glomerulosclerosis FSGS
|
|
Apoptosis
|
|
Alpha 6 Beta 4 signaling pathway
|
|
BDNF signaling pathway
|
|
Oncostatin M Signaling Pathway
|
|
Corticotropin-releasing hormone
|
|
Interleukin-11 Signaling Pathway
|
|
TNF alpha Signaling Pathway
|
|
B Cell Receptor Signaling Pathway
|
|
Prostate Cancer
|
|
TSLP Signaling Pathway
|
|
IL17 signaling pathway
|
|
IL-7 Signaling Pathway
|
|
Regulation of Microtubule Cytoskeleton
|
|
TWEAK Signaling Pathway
|
|
FSH signaling pathway
|
|
TSH signaling pathway
|
|
RANKL/RANK Signaling Pathway
|
|
SREBP signalling
|
|
Integrated Cancer pathway
|
|
IL-1 signaling pathway
|
|
Metabolism of nitric oxide
|
|
Integrin-mediated Cell Adhesion
|
|
TFs Regulate miRNAs related to cardiac hypertrophy
|
|
MicroRNAs in cardiomyocyte hypertrophy
|
|
Angiogenesis
|
|
TOR Signaling
|
|
Regulation of toll-like receptor signaling pathway
|
|
AMPK Signaling
|
|
Androgen receptor signaling pathway
|
|
IL-5 Signaling Pathway
|
| References |
| REF 1 | Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000 Apr 6;43(7):1380-97. |
|---|
| 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: 5675). |
|---|
| 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. |
|---|
| REF 4 | A phase I clinical and pharmacokinetic study of oral CI-1033 in combination with docetaxel in patients with advanced solid tumors. Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4274-82. |
|---|
