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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
CRIZOTINIB

CRIZOTINIB


ATC L01ED01

ANTINEOPLASTIC AGENTS
TYROSINE KINASE INHIBITOR

ORAL

F 43 PERCENT (250 MILLIGRAM)

VD 1772 LITER (50 MILLIGRAM INTRAVENOUS)

PPB 91 PERCENT

Cl 60 LITER / HOUR (500 MILLIGRAM DAILY)

HT 42 HOUR (250 MILLIGRAM)

SOLUBILITY IN AQUEOUS MEDIA DECREASES OVER THE RANGE PH 1.6 TO PH 8.2 FROM GREATER THAN 10 MILLIGRAM / MILLILITER TO LESS THAN 0.1 MILLIGRAM / MILLILITER

TYROSINE KINASES
ALK (IC50=24 NANOMOLAR) PMID22162641
C-MET

PDB 5AAB (STRUCTURE OF C1156Y,L1198F MUTANT HUMAN ANAPLASTIC LYMPHOMA KINASE IN COMPLEX WITH CRIZOTINIB)

LIGAND CODE = VGH (link to the list of PDB complexes)

Download experimental 3D coordinates of VGH with added hydrogens

Hepatocyte growth factor receptor UNIPROT P08581 MET -- ALK tyrosine kinase receptor UNIPROT Q9UM73 ALK

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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