|
gptkbp:instance_of
|
gptkb:Atom
|
|
gptkbp:administered_by
|
oral tablet
|
|
gptkbp:approves
|
gptkb:European_Union
gptkb:United_States
|
|
gptkbp:casnumber
|
675576-98-4
|
|
gptkbp:chemical_formula
|
C16 H18 N4 O3 S
|
|
gptkbp:class
|
piperazine derivative
|
|
gptkbp:clinical_trial
|
gptkb:Europe
gptkb:Asia
gptkb:USA
Phase I
|
|
gptkbp:composed_by
|
gptkb:chemical_compound
|
|
gptkbp:developed_by
|
gptkb:Oncology
gptkb:Kaposi's_sarcoma
gptkb:neuroblastoma
|
|
gptkbp:discovered_by
|
gptkb:Hoffmann-La_Roche
|
|
gptkbp:dissolved
|
insoluble in water
soluble in DMSO
soluble in ethanol
|
|
gptkbp:first_described_by
|
gptkb:2004
|
|
https://www.w3.org/2000/01/rdf-schema#label
|
nutlin-3
|
|
gptkbp:invention
|
patented
|
|
gptkbp:investigates
|
solid tumors
hematological malignancies
metastatic cancers
pediatric cancers
adult cancers
|
|
gptkbp:knockouts
|
high affinity for MDM2
|
|
gptkbp:marketed_as
|
trade name Nutlin-3a
|
|
gptkbp:mechanism_of_action
|
inhibits MDM2-p53 interaction
|
|
gptkbp:pharmacokinetics
|
cell cycle arrest
oral bioavailability
p53 reactivation
metabolized in liver
half-life of 4-6 hours
induction of apoptosis
inhibition of cell proliferation
|
|
gptkbp:related_products
|
gptkb:nutlin-3a
gptkb:nutlin-3b
gptkb:nutlin-4
|
|
gptkbp:related_to
|
p53 tumor suppressor protein
|
|
gptkbp:research_focus
|
apoptosis
cell cycle regulation
oncology
drug resistance
tumor biology
|
|
gptkbp:safety_features
|
generally well tolerated
|
|
gptkbp:side_effect
|
gptkb:anemia
fatigue
nausea
diarrhea
|
|
gptkbp:targets
|
gptkb:MDM2
|
|
gptkbp:used_for
|
gptkb:cancer_treatment
|
|
gptkbp:bfsParent
|
gptkb:MDM2
|
|
gptkbp:bfsLayer
|
5
|