General
Preferred name
AXITINIB
Synonyms
AG-013736 ()
AG-013736, Inlyta, AG-13736 ()
AG 013736 ()
Indazole derivative 5 ()
Axitinib (AG 013736) ()
AG-013736AxitinibS1005 ()
AG-13736 ()
INLYTA ()
NSC-757441 ()
PF-06778691 ()
Axitinib-13C-d3 ()
P&D ID
PD003467
CAS
319460-85-0
1261432-00-1
Tags
available
drug
obsolete probe
Approved by
FDA
First approval
2012
Drug indication
Renal cell carcinoma
Neoplasm
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)
ROE Axitinib is mainly eliminated unchanged in the feces (41%) with 12% of the original dose as unchanged axitinib. There is also 23% eliminated in the urine, most of which are metabolites.; ;
ABSORPTION After one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration.; ;
METABOLISM Axitinib undergoes mainly hepatic metabolism. CYP3A4 and CYP3A5 are the main hepatic enzymes while CYP1A2, CYP2C19, and UGT1A1 enzymes are secondary.; ;
DESCRIPTION Axitinib is a Type-1 kinase inhibitor. Axitinib inhibits several receptor tyrosine kinases including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT. (GtoPdb)
DESCRIPTION Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFR¦Â, respectively.
PRICE 29
DESCRIPTION Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFR?? (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.
DESCRIPTION inhibitor of VEGFRs, c-KIT, and PDGFR alpha and beta (Informer Set)
DESCRIPTION Used in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer. (PKIDB)
DESCRIPTION Potent and selective GSK-3beta inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Potent VEGFR-1, -2 and -3 inhibitor (Tocriscreen Plus)
DESCRIPTION Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma. (TargetMol Bioactive Compound Library)
Cell lines
473
Organisms
0
Compound Sets
34
AdooQ Bioactive Compound Library
A10103
Axon Medchem Screening Library
1414
Cayman Chemical Bioactives
13813
26676
ChEMBL Approved Drugs
CHEMBL1289926
ChEMBL Drugs
CHEMBL1289926
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5659
Concise Guide to Pharmacology 2019/20
5659
Concise Guide to Pharmacology 2021/22
5659
Concise Guide to Pharmacology 2023/24
5659
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB06626
DrugBank Approved Drugs
DB06626
DrugCentral
4225
DrugCentral Approved Drugs
4225
DrugMAP
DMGVH6N
DMM1I8R
DrugMAP Approved Drugs
DMGVH6N
Enamine Bioactive Compounds
EBC-575146
Guide to Pharmacology
5659
Informer Set
348990
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1289926
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1289926
MedChem Express Bioactive Compound Library
HY-10065
NCATS Inxight Approved Drugs
C9LVQ0YUXG
NIH Approved Oncology Drugs
144075334
Obsolete Compounds
axitinib
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Axitinib
TargetMol Bioactive Compound Library
T1452
Tocris Bioactive Compound Library
4350
Tocriscreen Plus
4350
Welcome Trust Cancer Drugs
1021
External IDs
41
Properties
(calculated by RDKit )
Molecular Weight
386.12
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
4
cLogP
4.64
TPSA
70.67
Fraction CSP3
0.05
Chiral centers
0.0
Largest ring
6.0
QED
0.52
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target
FLT1
FLT3
KDR
KIT
PDGFRA
PDGFRB
PDGFR, KIT, VEGFR
c-Kit
PDGFR
PDGFRβ
VEGFR
VEGFR1
VEGFR2
VEGFR3
CSF1, FLT1, FLT4, KDR, PLK4
VEGFR inhibitor
c-Kit,PDGFR,VEGFR
FLT4
Compound status
FDA
Target Type
Enzyme-Linked Receptors
Pathway
RTK signaling
Angiogenesis
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Targets
FLT1,KDR,FLT4
MOA
Inhibitor
PDGFR tyrosine kinase receptor inhibitor, VEGFR inhibitor
Indication
renal cell carcinoma (RCC)
Therapeutic Class
Anticancer Agents
Source data