Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:216239
Structure:
Synonyms:
2-Pyridinecarboxamide, 4-(4-((((4-chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy)-N-methyl-
284461-73-0
4-(4-((((4-Chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy)-N-methyl-2-pyridinecarboxamide
4-(4-(3-(4-chloro-3-trifluoromethylphenyl)ureido)phenoxy)pyridine-2-carboxyllic acid methyamide-4-methylbenzenesulfonate
4-(4-{3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido}phenoxy)-N(sup 2)-methylpyridine-2-carboxamide
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-pyridine-2-carboxamide
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
4-{4-[({[4-CHLORO-3-(TRIFLUOROMETHYL)PHENYL]AMINO}CARBONYL)AMINO]PHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE
BAX
BAY 43-9006
BAY 439006
BAY-43-0006
BAY-43-9006
BAY-54-9085
CHEBI:50924
DB00398
K00597a
LS-186067
LS-187021
LS-187788
N-(4-Chloro-3-(trifluoromethyl)phenyl)-N'-(4-(2-(N-methylcarbamoyl)-4-pyri
N-(4-Chloro-3-(trifluoromethyl)phenyl)-N'-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea
NCGC00167488-01
nchembio.117-comp17
Nexavar
NSC-724772
Sorafenib
Sorafenib tosylate
Sorafenib [INN]
sorafenibum
STOCK6S-50043
ZINC01493878
ATC-Codes:
Side-Effects:
Side-EffectFrequency
weight loss0
influenza0
mediastinal disorders0
cholangitis0
heart disease0
hypothyroidism0
abdominal pain upper0
exfoliative dermatitis0
dyspepsia0
peripheral edema0
puncture0
breast disorders0
acute renal failure0
keratoacanthomas0
rash0
atopic dermatitis0
constipation0
folliculitis0
hematuria0
heart failure0
congestive heart failure0
stomatitis0
dry skin0
ulcer0
vascular disorders0
thrombocythemia0
infection0
gynecomastia0
amylase increased0
abdominal pain0
cerebral hemorrhage0
dyspnea0
vomiting0
neuropathy0
myalgia0
loss of consciousness0
arthralgia0
hypotension0
headache0
dehydration0
neutropenia0
connective tissue disorders0
erythema multiforme0
hematoma0
constitutional symptoms0
tachycardia0
pancreatitis0
proteinuria0
interstitial nephritis0
epistaxis0
thrombocytopenia0
hemorrhage0
mood alteration0
malaise0
gastritis0
dry mouth0
anemia0
jaundice0
dysphagia0
arrhythmia0
cancer0
gastroesophageal reflux0
gum hemorrhage0
pain0
pain in limb0
nausea0
transient ischemic attack0
urticaria0
erythema0
cholecystitis0
rectal hemorrhage0
esophageal varices0
fever0
acne0
hematemesis0
nephrotic syndrome0
hypertension0
lymphopenia0
pruritus0
syncope0
eczema0
renal failure0
hoarseness0
fatigue0
rhinorrhea0
endocrine disorders0
asthenia0
diarrhea0
tinnitus0
myocardial ischemia0
intracranial hemorrhage0
hemoptysis0
ascites0
dizziness0
edema0
menorrhagia0
anorexia0
hyponatremia0
hypophosphatemia0
pleural effusion0
flushing0
tumor0
leukopenia0
alopecia0
cough0
hypersensitivity0
glossodynia0

Target

show target details
Uniprot ID:RAF1_MOUSE
Synonyms:
C-RAF
cRaf
RAF proto-oncogene serine/threonine-protein kinase
Raf-1
EC-Numbers:2.7.11.1
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

15466206
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.. Scott M Wilhelm; Christopher Carter; Liya Tang; Dean Wilkie; Angela McNabola; Hong Rong; Charles Chen; Xiaomei Zhang; Patrick Vincent; Mark McHugh; Yichen Cao; Jaleel Shujath; Susan Gawlak; Deepa Eveleigh; Bruce Rowley; Li Liu; Lila Adnane; Mark Lynch; Daniel Auclair; Ian Taylor; Rich Gedrich; Andrei Voznesensky; Bernd Riedl; Leonard E Post; Gideon Bollag; Pamela A Trail (2004) Cancer research display abstract
The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. The novel bi-aryl urea BAY 43-9006 is a potent inhibitor of Raf-1, a member of the RAF/MEK/ERK signaling pathway. Additional characterization showed that BAY 43-9006 suppresses both wild-type and V599E mutant BRAF activity in vitro. In addition, BAY 43-9006 demonstrated significant activity against several receptor tyrosine kinases involved in neovascularization and tumor progression, including vascular endothelial growth factor receptor (VEGFR)-2, VEGFR-3, platelet-derived growth factor receptor beta, Flt-3, and c-KIT. In cellular mechanistic assays, BAY 43-9006 demonstrated inhibition of the mitogen-activated protein kinase pathway in colon, pancreatic, and breast tumor cell lines expressing mutant KRAS or wild-type or mutant BRAF, whereas non-small-cell lung cancer cell lines expressing mutant KRAS were insensitive to inhibition of the mitogen-activated protein kinase pathway by BAY 43-9006. Potent inhibition of VEGFR-2, platelet-derived growth factor receptor beta, and VEGFR-3 cellular receptor autophosphorylation was also observed for BAY 43-9006. Once daily oral dosing of BAY 43-9006 demonstrated broad-spectrum antitumor activity in colon, breast, and non-small-cell lung cancer xenograft models. Immunohistochemistry demonstrated a close association between inhibition of tumor growth and inhibition of the extracellular signal-regulated kinases (ERKs) 1/2 phosphorylation in two of three xenograft models examined, consistent with inhibition of the RAF/MEK/ERK pathway in some but not all models. Additional analyses of microvessel density and microvessel area in the same tumor sections using antimurine CD31 antibodies demonstrated significant inhibition of neovascularization in all three of the xenograft models. These data demonstrate that BAY 43-9006 is a novel dual action RAF kinase and VEGFR inhibitor that targets tumor cell proliferation and tumor angiogenesis.