General
Preferred name
TIVOZANIB
Synonyms
AV-951 ()
KRN951 ()
AV-951 (hydrochloride hydrate) ()
KRN951 (hydrochloride hydrate) ()
AV-951, KRN-951, Kil8951, Tivozanib HCl, Kil-8951, ASP-4130 ()
Tivozanib (AV-951) ()
Tivozanib (hydrochloride hydrate) ()
tivozanib (ophthalmic), Ophthotech ()
ASP-4130 ()
FOTIVDA ()
KIL-8951 ()
KIL8951 ()
KRN-951 ()
Tivozanib hydrate ()
(tivozanib hydrochloride hydrate ()
Tivozanib hydrochloride monohydrate ()
TIVOZANIB HYDROCHLORIDE ()
Tivozanib (hydrate) ()
P&D ID
PD003428
CAS
475108-18-0
682745-41-1
682745-40-0
Tags
available
probe
drug
Approved by
EMA
FDA
First approval
2017
Drug indication
Renal cell carcinoma
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
experimental probe
Probe sources
Chemical Probes.org
Probe targets
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 Tivozanib is an oral VEGF receptor tyrosine kinase inhibitor. (GtoPdb)
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION inhibitor of VEGFRs (Informer Set)
DESCRIPTION On March 2021, FDA approved tivozanib to treat patients with renal cell carcinoma (PKIDB)
DESCRIPTION Tivozanib is an orally available VEGFR inhibitor with IC50 values of 0.21, 0.16, and 0.24 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. It has been improved for the treatment of renal cell carcinoma. It also displays activity against other cancers. (BOC Sciences Bioactive Compounds)
Cell lines
1
Organisms
0
Compound Sets
31
AdooQ Bioactive Compound Library
A10101
Axon Medchem Screening Library
1717
BOC Sciences Bioactive Compounds
tivozanib-hydrate-cas-682745-40-0-8877
Cayman Chemical Bioactives
18493
ChEMBL Approved Drugs
CHEMBL1289494
CHEMBL2105756
ChEMBL Drugs
CHEMBL1289494
CHEMBL2105756
Chemical Probes.org
krn-951
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB11800
DrugBank Approved Drugs
DB11800
DrugCentral
5258
DrugCentral Approved Drugs
5258
DrugMAP
DMUKC5L
DrugMAP Approved Drugs
DMUKC5L
EU-OPENSCREEN Bioactive Compound Library
EOS101098
EUbOPEN Chemogenomics Library
EUB0000661
Guide to Pharmacology
6058
Informer Set
418170
LINCS compound set
10005-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1289494
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1289494
MedChem Express Bioactive Compound Library
HY-10977
HY-10977A
NCATS Inxight Approved Drugs
172030934T
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
AV-951
TargetMol Bioactive Compound Library
T2456
Welcome Trust Cancer Drugs
312
External IDs
47
Properties
(calculated by RDKit )
Molecular Weight
454.1
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
4
cLogP
5.64
TPSA
107.74
Fraction CSP3
0.14
Chiral centers
0.0
Largest ring
6.0
QED
0.39
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
FLT1
FLT3
KDR
VEGFR
EphB2
PDGFR??
VEGFR1
VEGFR2
VEGFR3
FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
FLT4
c-Kit,PDGFR,VEGFR
FLT1, KDR, FLT4
Compound status
clinical
Pathway
RTK signaling
Angiogenesis
Tyrosine Kinase/Adaptors
Chromatin/Epigenetic
Protein Tyrosine Kinase/RTK
Targets
FLT1,KDR,FLT4
Member status
member
MOA
VEGFR-1 (Flt-1) Inhibitors
VEGFR-2 (FLK-1/KDR) Inhibitors
VEGFR-3 (FLT4) Inhibitors
Angiogenesis Inhibitors
VEGFR inhibitor
Indication
renal cell carcinoma (RCC)
Target class
Kinase, Kinase, Kinase
Target subclass
Tyrosine kinase, Tyrosine kinase, Tyrosine kinase
Recommended Cell Concentration
None
Source data