General
Preferred name
CRIZOTINIB
Synonyms
Xalkori, PF-2341066 ()
PF02341066 ()
PF-02341066 hydrochloride ()
PF-02341066 ()
Crizotinib hydrochloride ()
PF-2341066 (Crizotinib) ()
PF 02341066 ()
PF-2341066 ()
XALKORI ()
S1068 ()
Crizotinib (hydrochloride) ()
NSC-756645 ()
PF-02341066 (hydrochloride) ()
Crizotinib (PF-02341066) ()
Xalkori, PF-02341066 hydrochloride ()
(R)-Crizotinib ()
(R)-Crizotinib-d5 ()
P&D ID
PD003326
CAS
877399-52-5
1415560-69-8
1395950-84-1
Tags
obsolete probe
natural product
drug
available
Approved by
EMA
FDA
First approval
2011
Drug Status
investigational
approved
Drug indication
Non-small-cell lung cancer
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Critzotinib is a Type-1 kinase inhibitor and was first approved by the FDA in 2011. It inhibits ALK, cMET and ROS1 receptor tyrosine kinases. Critzotinib is a chiral molecule that exploits the three-dimensional space of the ATP pocket to achieve optimal potency and selectivity . The R-enantiomer as shown here exhibits better potency than the either the racemate or S-isomer and the approved drug should contain only the R-enantiomer.
Pfizer developed the 3rd generation ALK inhibitor as a follow-up to critzotinib, and this new drug has been reported to outperfom its predecessor in lung cancer. (GtoPdb)
Pfizer developed the 3rd generation ALK inhibitor as a follow-up to critzotinib, and this new drug has been reported to outperfom its predecessor in lung cancer. (GtoPdb)
DESCRIPTION
Crizotinib is used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic-lymphoma kinase (ALK)-positive as detected by a FDA-approved test.
(PKIDB)
DESCRIPTION
inhibitor of c-MET and ALK
(Informer Set)
DESCRIPTION
Selective urokinase (uPA) inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM). Crizotinib is useful in treatment of anaplastic large-cell lymphoma.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
218
Organisms
0
Compound Sets
33
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine BioReference Compounds
Guide to Pharmacology
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Obsolete Compounds
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
43
Molecular Weight
449.12
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
3
cLogP
5.04
TPSA
77.99
Fraction CSP3
0.33
Chiral centers
1.0
Largest ring
6.0
QED
0.53
Structural alerts
3
aggregator (ZINC)
Aggregators
aggregator (Aggregator Advisor)
Aggregators
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target
ALK
MET
c-Met
ALK, MET
MET/ALK inhibitor
Anaplastic lymphoma kinase (ALK)
ROS Kinase
ALK,Autophagy,c-Met,ROS1
Compound status
FDA
Targets
MET,ALK
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Autophagy
Protein Tyrosine Kinase/RTK
MOA
c-Met/HGFR
Inhibitor
ALK tyrosine kinase receptor inhibitor
Indication
non-small cell lung cancer (NSCLC)
Source data
