General
Preferred name
AXITINIB
Synonyms
AG-013736 ()
AG-013736, Inlyta, AG-13736 ()
AG 013736 ()
S1005 ()
Indazole derivative 5 ()
AG-13736 ()
INLYTA ()
NSC-757441 ()
Axitinib (AG 013736) ()
Axitinib-13C-d3 ()
P&D ID
PD003467
CAS
319460-85-0
1261432-00-1
Tags
obsolete probe
natural product
drug
available
Approved by
FDA
First approval
2012
Drug Status
investigational
approved
Drug indication
Renal cell carcinoma
Max Phase
Phase 4
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 Used in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer. (PKIDB)
DESCRIPTION inhibitor of VEGFRs, c-KIT, and PDGFR alpha and beta (Informer Set)
DESCRIPTION Potent and selective GSK-3beta inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Potent VEGFR-1, -2 and -3 inhibitor (Tocriscreen Plus)
Cell lines
472
Organisms
0
Compound Sets
32
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
Drug Repurposing Hub
DrugBank
DB06626
DrugBank Approved Drugs
DB06626
DrugCentral
4225
DrugCentral Approved Drugs
4225
DrugMAP
DMGVH6N
DMM1I8R
DrugMAP Approved Drugs
DMGVH6N
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
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
37
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
PDGFR??
VEGFR1
VEGFR2
VEGFR3
c-Kit
CSF1, FLT1, FLT4, KDR, PLK4
VEGFR inhibitor
FLT4
c-Kit,PDGFR,VEGFR
Compound status
FDA
Target Type
Enzyme-Linked Receptors
Pathway
RTK signaling
Angiogenesis
Tyrosine Kinase/Adaptors
Chromatin/Epigenetic
Protein Tyrosine Kinase/RTK
Targets
FLT1,KDR,FLT4
Primary Target
VEGFR
MOA
PDGFR
Inhibitor
PDGFR tyrosine kinase receptor inhibitor, VEGFR inhibitor
Indication
renal cell carcinoma (RCC)
Therapeutic Class
Anticancer Agents
Source data