General
Preferred name
ORANTINIB
Synonyms
SU 6668 ()
TSU-68, SU-6668 ()
SU6668 ()
TSU-68 ()
NSC 702827 ()
TSU-68 (SU6668) ()
Rosiglitazone + metformin ()
(Z)-Orantinib ()
(Z)-SU6668 ()
(Z)-TSU-68 ()
NSC-702827 ()
SU-6668 ()
Orantinib (SU6668) ()
Su006668 ()
SU-006668 ()
P&D ID
PD011179
CAS
252916-29-3
210644-62-5
Tags
available
drug candidate
Drug indication
Neoplasm
Diabetic complication
Advanced solid tumour
Drug Status
investigational
Max Phase
3.0
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
Orantinib is a multi-kinase inhibitor.
(GtoPdb)
DESCRIPTION
Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 ¦ÌM, 8 nM and 1.2 ¦ÌM for Flt-1, PDGFR¦Â and FGFR1, respectively.
DESCRIPTION
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk©\1/KDR, PDGFR¦Â, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 ¦ÌM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors[1][2].
PRICE
53
DESCRIPTION
Potent AMPK activator
(Tocris Bioactive Compound Library)
DESCRIPTION
PDGFR, VEGFR and FGFR inhibitor
(Tocriscreen Plus)
DESCRIPTION
PDGFR, VEGFR and FGFR inhibitor
(Tocriscreen Total)
DESCRIPTION
Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
23
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
JUMP-Target 1 Compound Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
PKIDB
Probe Miner (suitable probes)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
62
Molecular Weight
310.13
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
3
Rotatable Bonds
4
Ring Count
3
Aromatic Ring Count
2
cLogP
3.14
TPSA
82.19
Fraction CSP3
0.22
Chiral centers
0.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
PDGFRA,PDGFRB
Target Type
Enzyme-Linked Receptors
Target
Apoptosis
FGFR
FGFR1
Flk1
PDGFR
PDGFRβ
VEGFR
PDGFR¦Â
AURKA, AURKB, EGFR, FGFR1, FGFR2, KDR, PDGFRA, PDGFRB
RTK inhibitor
AURKB
KDR
PDGFRB
MOA
PDGFR inhibitor
Inhibitor
FGFR inhibitor, PDGFR tyrosine kinase receptor inhibitor, VEGFR inhibitor
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Source data
