General
Preferred name
CRIZOTINIB
Synonyms
Xalkori, PF-2341066 ()
PF02341066 ()
PF-02341066 ()
PF-02341066 hydrochloride ()
PF-2341066 (Crizotinib) ()
Crizotinib hydrochloride ()
PF 02341066 ()
Crizotinib (hydrochloride) ()
PF-02341066 (hydrochloride) ()
Xalkori, PF-02341066 hydrochloride ()
Crizotinib (PF-02341066) ()
PF-2341066CrizotinibXalkoriS1068 ()
NSC-756645 ()
PF-2341066 ()
XALKORI ()
(R)-Crizotinib ()
(R)-Crizotinib-d5 ()
P&D ID
PD003326
CAS
877399-52-5
1415560-69-8
1395950-84-1
Tags
available
drug
obsolete probe
Approved by
FDA
EMA
First approval
2011
Drug indication
Non-small-cell lung cancer
Glioblastoma multiforme
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.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)
DESCRIPTION Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition[1][2][3].
PRICE 38
DESCRIPTION Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition[1][2][3].
PRICE 47
DESCRIPTION inhibitor of c-MET and ALK (Informer Set)
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 Selective urokinase (uPA) inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Crizotinib is a receptor tyrosine kinase inhibitor used to treat metastatic non-small cell lung cancer (NSCLC) where the tumors have been confirmed to be anaplastic lymphoma kinase (ALK), or ROS1-positive. (Enamine Bioactive Compounds)
DESCRIPTION Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors. (TargetMol 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)
DESCRIPTION Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met, with IC50 values of 20 nM and 8 nM, respectively. (TargetMol Bioactive Compound Library)
Cell lines
232
Organisms
1
Compound Sets
34
AdooQ Bioactive Compound Library
A10712
A16245
Axon Medchem Screening Library
1660
BOC Sciences Bioactive Compounds
crizotinib-hydrochloride-cas-1415560-69-8-item-84-463226
Cayman Chemical Bioactives
12087
26762
ChEMBL Approved Drugs
CHEMBL601719
ChEMBL Drugs
CHEMBL601719
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
4903
Concise Guide to Pharmacology 2019/20
4903
Concise Guide to Pharmacology 2021/22
4903
Concise Guide to Pharmacology 2023/24
4903
Drug Repurposing Hub
DrugBank
DB08865
DrugBank Approved Drugs
DB08865
DrugCentral
4187
DrugCentral Approved Drugs
4187
DrugMAP
DM4F29C
DrugMAP Approved Drugs
DM4F29C
Enamine Bioactive Compounds
EBC-12789
EBC-564177
Enamine BioReference Compounds
Guide to Pharmacology
4903
Informer Set
628603
LINCS compound set
10027-101
10027-999
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL601719
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL601719
MedChem Express Bioactive Compound Library
HY-50878
HY-50878A
NCATS Inxight Approved Drugs
53AH36668S
NIH Approved Oncology Drugs
131408690
Obsolete Compounds
crizotinib
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
PF-2341066
crizotinib-hydrochloride
TargetMol Bioactive Compound Library
T1661
T8399
Tocris Bioactive Compound Library
4368
External IDs
49
Properties
(calculated by RDKit )
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 (Aggregator Advisor)
Aggregators
historic compounds (Chemical Probes.org)
Obsolete
aggregator (ZINC)
Aggregators
Related compounds
Custom attributes
(extracted from source data)
Target
ALK
MET
ALK, MET
MET/ALK inhibitor
Anaplastic lymphoma kinase (ALK)
ROS Kinase
ALK,Autophagy,c-Met,ROS1
c-Met
ROS
Ros1
Compound status
FDA
Targets
MET,ALK
Pathway
Angiogenesis
Autophagy
Immunology/Inflammation
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
MOA
c-Met/HGFR
Inhibitor
ALK tyrosine kinase receptor inhibitor
Indication
non-small cell lung cancer (NSCLC)
Source data