General
Preferred name
SUNITINIB
Synonyms
SUNITINIB MALATE ()
Sutent ()
NSC750690 ()
SU-11248, Sutent, Sunitinib Malate ()
SU 11248 ()
SU 11248 (Malate) ()
SU 11248 (Malate)SU 11248 ()
PMID28460551-Compound-2 ()
Sunitinib (malate) ()
SU11248 ()
Sunitinib (SU11248) malate ()
Sunitinib (SU11248) ()
Sunitinib (free base)Sutent (free base)Sunitinib (free base)1H-Pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-Pyrrole-3-carboxamide,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl- ()
NSC-736511 ()
NSC-750690 ()
SU-011248 ()
SU-11248 ()
SU011248 ()
SUNITINIB ACCORD ()
Sunitinib-d10 ()
Sunitinib accord ()
SU010398 ()
SU-010398 ()
PHA-290940AD ()
Sunitinib l-malate ()
SU011248 L-MALATE SALT ()
SU-011248 L-MALATE SALT ()
P&D ID
PD003663
CAS
557795-19-4
341031-54-7
1126641-10-8
1126721-82-1
Tags
available
covalent binder
nuisance
drug
obsolete probe
Approved by
FDA
EMA
First approval
2006
Drug indication
Gastrointestinal stromal tumour
Gastrointestinal cancer
Gastrointestinal stromal tumor
Neoplasm
non-small cell lung carcinoma
Renal cell carcinoma
Drug Status
approved
investigational
Max Phase
4.0
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
Sunitinib is a Type-1 kinase inhibitor and was first approved by the US FDA and EMA in 2006.
(GtoPdb)
PRICE
29
DESCRIPTION
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFR¦Â, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1¦Á by inhibiting autophosphorylation and consequent RNase activation[2].
DESCRIPTION
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFR?? (IC50=80/2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.
DESCRIPTION
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFR¦Â, respectively[1]. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1¦Á by inhibiting autophosphorylation and consequent RNase activation[2].
PRICE
29
DESCRIPTION
Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFR?? (IC50: 80/2 nM), and c-kit.
DESCRIPTION
inhibitor of VEGFRs, c-KIT, and PDGFR alpha and beta
(Informer Set)
DESCRIPTION
For the treatment of advanced renal cell carcinoma as well as the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate.
(PKIDB)
DESCRIPTION
Sunitinib is a small-molecule multi-targeted receptor tyrosine kinase inhibitor. It is used fhe treatment of advanced renal cell carcinoma as well as the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate.
(Enamine Bioactive Compounds)
DESCRIPTION
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Broad spectrum MMP inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Potent VEGFR, PDGFRbeta and KIT inhibitor
(Tocriscreen Plus)
DESCRIPTION
Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
303
Organisms
11
Compound Sets
45
Axon Medchem Screening Library
Bioprocess diversity set
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CovalentInDB
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
Enamine Bioactive Compounds
Enamine BioReference Compounds
Guide to Pharmacology
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Nuisance compounds in cellular assays
Obsolete Compounds
PKIDB
Reference compounds for characterizing cellular injury in high-content cellular morphology assays
ReFrame library
Selleckchem Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
77
Molecular Weight
398.21
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
3
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
2
cLogP
3.33
TPSA
77.23
Fraction CSP3
0.36
Chiral centers
0.0
Largest ring
6.0
QED
0.63
Structural alerts
2
historic compounds (Chemical Probes.org)
Obsolete
Nonspecific kinase inhibition
Nuisance compounds
Related compounds
Custom attributes
(extracted from source data)
Target
FLT1
FLT3
KDR
KIT
PDGFRA
PDGFRB
Tyrosine-protein kinase receptor FLT3
PDGFRA, PDGFRB, KDR, KIT, FLT3
Vascular endothelial growth factor receptor
Platelet-derived growth factor receptor
Stem cell growth factor receptor
Tyrosine-protein kinase receptor RET
Macrophage colony stimulating factor receptor
PDGFR¦Â
VEGFR2
CSF1R, FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB, RET
PDGFR inhibitor
Apoptosis related,c-Kit,IRE1,Mitophagy,PDGFR,VEGFR
Apoptosis related,Autophagy,c-Kit,IRE1,PDGFR,VEGFR
FLT4
CSF1R
IRE1
Mitophagy
PDGFRβ
Compound status
FDA
Target Type
Enzyme-Linked Receptors
Pathway
RTK signaling
Angiogenesis
Apoptosis
Autophagy
Cell Cycle/Checkpoint
Tyrosine Kinase/Adaptors
Cell Cycle/DNA Damage
Protein Tyrosine Kinase/RTK
Biological process
Mitosis & chromosome segregation
MOA
receptor protein-tyrosine kinase inhibitor
c-Kit
FLT
PDGFR
Inhibitor
FLT3 inhibitor, KIT inhibitor, PDGFR tyrosine kinase receptor inhibitor, RET tyrosine kinase inhibitor, VEGFR inhibitor
Targets
KDR,PDGFRB
Primary Target
VEGFR
Member status
member
Indication
gastrointestinal stromal tumors (GIST), renal cell carcinoma (RCC), neuroendocrine tumors of pancreatic origin (PNET)
Cellular injury category
Kinase
Therapeutic Class
Anticancer Agents
VGSC Target
Nav1.5
Source data
