Hmdb loader
Survey
You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on Human Metabolome Database.
Record Information
Version5.0
StatusExpected but not Quantified
Creation Date2012-09-06 15:16:52 UTC
Update Date2022-03-07 02:51:58 UTC
HMDB IDHMDB0015397
Secondary Accession Numbers
  • HMDB15397
Metabolite Identification
Common NameSunitinib
DescriptionSunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and flt3.
Structure
Data?1582753292
Synonyms
ValueSource
SU-11248ChEBI
SunitinibumChEBI
SutentChEBI
SU11248HMDB
Sunitinib malateHMDB
5-(5-Fluoro-2-oxo-1,2-dihydroindolylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amideHMDB
Chemical FormulaC22H27FN4O2
Average Molecular Weight398.4738
Monoisotopic Molecular Weight398.211804333
IUPAC NameN-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide
Traditional Namesunitinib
CAS Registry Number557795-19-4
SMILES
CCN(CC)CCNC(=O)C1=C(C)NC(\C=C2/C(=O)NC3=C2C=C(F)C=C3)=C1C
InChI Identifier
InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChI KeyWINHZLLDWRZWRT-ATVHPVEESA-N
Chemical Taxonomy
Description Belongs to the class of organic compounds known as indolines. Indolines are compounds containing an indole moiety, which consists of pyrrolidine ring fused to benzene to form 2,3-dihydroindole.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassIndolines
Direct ParentIndolines
Alternative Parents
Substituents
  • Dihydroindole
  • Pyrrole-3-carboxamide
  • Pyrrole-3-carboxylic acid or derivatives
  • Aryl fluoride
  • Aryl halide
  • Substituted pyrrole
  • Benzenoid
  • Pyrrole
  • Heteroaromatic compound
  • Vinylogous amide
  • Tertiary amine
  • Amino acid or derivatives
  • Secondary carboxylic acid amide
  • Tertiary aliphatic amine
  • Carboxamide group
  • Lactam
  • Azacycle
  • Carboxylic acid derivative
  • Amine
  • Organofluoride
  • Organohalogen compound
  • Organonitrogen compound
  • Organopnictogen compound
  • Organooxygen compound
  • Organic oxide
  • Carbonyl group
  • Organic oxygen compound
  • Organic nitrogen compound
  • Hydrocarbon derivative
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Ontology
Physiological effectNot Available
Disposition
ProcessNot Available
RoleNot Available
Physical Properties
StateSolid
Experimental Molecular Properties
PropertyValueReference
Melting PointNot AvailableNot Available
Boiling PointNot AvailableNot Available
Water Solubility0.031 g/LNot Available
LogP2.5Not Available
Experimental Chromatographic PropertiesNot Available
Predicted Molecular Properties
PropertyValueSource
Water Solubility0.031 g/LALOGPS
logP3.24ALOGPS
logP2.93ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)11.46ChemAxon
pKa (Strongest Basic)9.04ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area77.23 ŲChemAxon
Rotatable Bond Count7ChemAxon
Refractivity116.27 m³·mol⁻¹ChemAxon
Polarizability44.32 ųChemAxon
Number of Rings3ChemAxon
BioavailabilityYesChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted Chromatographic Properties

Predicted Collision Cross Sections

PredictorAdduct TypeCCS Value (Å2)Reference
DeepCCS[M+H]+207.2630932474
DeepCCS[M-H]-204.90230932474
DeepCCS[M-2H]-238.83630932474
DeepCCS[M+Na]+214.06530932474
AllCCS[M+H]+196.932859911
AllCCS[M+H-H2O]+194.232859911
AllCCS[M+NH4]+199.332859911
AllCCS[M+Na]+200.032859911
AllCCS[M-H]-200.432859911
AllCCS[M+Na-2H]-200.932859911
AllCCS[M+HCOO]-201.632859911

Predicted Kovats Retention Indices

Underivatized

MetaboliteSMILESKovats RI ValueColumn TypeReference
SunitinibCCN(CC)CCNC(=O)C1=C(C)NC(\C=C2/C(=O)NC3=C2C=C(F)C=C3)=C1C4771.5Standard polar33892256
SunitinibCCN(CC)CCNC(=O)C1=C(C)NC(\C=C2/C(=O)NC3=C2C=C(F)C=C3)=C1C3561.4Standard non polar33892256
SunitinibCCN(CC)CCNC(=O)C1=C(C)NC(\C=C2/C(=O)NC3=C2C=C(F)C=C3)=C1C3713.8Semi standard non polar33892256

Derivatized

Derivative Name / StructureSMILESKovats RI ValueColumn TypeReference
Sunitinib,1TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3452.8Semi standard non polar33892256
Sunitinib,1TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3335.7Standard non polar33892256
Sunitinib,1TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C4546.5Standard polar33892256
Sunitinib,1TMS,isomer #2CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C3544.6Semi standard non polar33892256
Sunitinib,1TMS,isomer #2CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C3429.0Standard non polar33892256
Sunitinib,1TMS,isomer #2CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C4484.6Standard polar33892256
Sunitinib,1TMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C3447.4Semi standard non polar33892256
Sunitinib,1TMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C3083.4Standard non polar33892256
Sunitinib,1TMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C4051.5Standard polar33892256
Sunitinib,2TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3438.2Semi standard non polar33892256
Sunitinib,2TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3457.2Standard non polar33892256
Sunitinib,2TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C4261.0Standard polar33892256
Sunitinib,2TMS,isomer #2CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3323.0Semi standard non polar33892256
Sunitinib,2TMS,isomer #2CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3166.5Standard non polar33892256
Sunitinib,2TMS,isomer #2CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3820.4Standard polar33892256
Sunitinib,2TMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C3448.6Semi standard non polar33892256
Sunitinib,2TMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C3240.2Standard non polar33892256
Sunitinib,2TMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C3777.5Standard polar33892256
Sunitinib,3TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3378.1Semi standard non polar33892256
Sunitinib,3TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3306.8Standard non polar33892256
Sunitinib,3TMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C3587.9Standard polar33892256
Sunitinib,1TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3666.9Semi standard non polar33892256
Sunitinib,1TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3519.3Standard non polar33892256
Sunitinib,1TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C4552.0Standard polar33892256
Sunitinib,1TBDMS,isomer #2CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C3710.1Semi standard non polar33892256
Sunitinib,1TBDMS,isomer #2CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C3629.0Standard non polar33892256
Sunitinib,1TBDMS,isomer #2CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C4483.1Standard polar33892256
Sunitinib,1TBDMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C3654.3Semi standard non polar33892256
Sunitinib,1TBDMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C3298.9Standard non polar33892256
Sunitinib,1TBDMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C4064.5Standard polar33892256
Sunitinib,2TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3787.9Semi standard non polar33892256
Sunitinib,2TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3818.4Standard non polar33892256
Sunitinib,2TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)NC3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C4325.8Standard polar33892256
Sunitinib,2TBDMS,isomer #2CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3713.6Semi standard non polar33892256
Sunitinib,2TBDMS,isomer #2CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3553.0Standard non polar33892256
Sunitinib,2TBDMS,isomer #2CCN(CC)CCN(C(=O)C1=C(C)[NH]C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3918.9Standard polar33892256
Sunitinib,2TBDMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C3819.6Semi standard non polar33892256
Sunitinib,2TBDMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C3624.3Standard non polar33892256
Sunitinib,2TBDMS,isomer #3CCN(CC)CCNC(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C3866.0Standard polar33892256
Sunitinib,3TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3903.1Semi standard non polar33892256
Sunitinib,3TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3840.7Standard non polar33892256
Sunitinib,3TBDMS,isomer #1CCN(CC)CCN(C(=O)C1=C(C)N([Si](C)(C)C(C)(C)C)C(/C=C2\C(=O)N([Si](C)(C)C(C)(C)C)C3=CC=C(F)C=C23)=C1C)[Si](C)(C)C(C)(C)C3779.6Standard polar33892256
Spectra

GC-MS Spectra

Spectrum TypeDescriptionSplash KeyDeposition DateSourceView
Predicted GC-MSPredicted GC-MS Spectrum - Sunitinib GC-MS (Non-derivatized) - 70eV, Positivesplash10-001r-9043000000-f9288d8cb7c447b10d862017-09-01Wishart LabView Spectrum
Predicted GC-MSPredicted GC-MS Spectrum - Sunitinib GC-MS (Non-derivatized) - 70eV, PositiveNot Available2021-10-12Wishart LabView Spectrum
Predicted GC-MSPredicted GC-MS Spectrum - Sunitinib GC-MS (Non-derivatized) - 70eV, PositiveNot Available2021-10-12Wishart LabView Spectrum

MS/MS Spectra

Spectrum TypeDescriptionSplash KeyDeposition DateSourceView
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 10V, Positive-QTOFsplash10-0002-0419000000-d91569989d4c1e438a582016-08-01Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 20V, Positive-QTOFsplash10-1039-4964000000-32cdbd9b3679f4b806d92016-08-01Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 40V, Positive-QTOFsplash10-00di-9740000000-14530852543a6132d98b2016-08-01Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 10V, Negative-QTOFsplash10-0002-0019000000-716107e6148bcb3af14c2016-08-03Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 20V, Negative-QTOFsplash10-052b-5398000000-e20fbe1cd3f11ad37acb2016-08-03Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 40V, Negative-QTOFsplash10-0006-9230000000-0d8caf257003c837c3d62016-08-03Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 10V, Positive-QTOFsplash10-0002-0009000000-c7521df282758983a81b2021-10-11Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 20V, Positive-QTOFsplash10-003r-0197000000-fc31f5a3f60673e3fb482021-10-11Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 40V, Positive-QTOFsplash10-0a4i-0293000000-c9aae10759016725c9322021-10-11Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 10V, Negative-QTOFsplash10-0002-0009000000-f6f1dd2f48935333770c2021-10-11Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 20V, Negative-QTOFsplash10-0002-2049000000-fe9e71e910a9eddb20232021-10-11Wishart LabView Spectrum
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - Sunitinib 40V, Negative-QTOFsplash10-052g-6194000000-ce0d447fabdb293e18132021-10-11Wishart LabView Spectrum
Biological Properties
Cellular Locations
  • Extracellular
  • Membrane
Biospecimen Locations
  • Blood
  • Urine
Tissue LocationsNot Available
Pathways
Normal Concentrations
BiospecimenStatusValueAgeSexConditionReferenceDetails
BloodExpected but not QuantifiedNot QuantifiedNot AvailableNot AvailableTaking drug identified by DrugBank entry DB01268 details
UrineExpected but not QuantifiedNot QuantifiedNot AvailableNot AvailableTaking drug identified by DrugBank entry DB01268 details
Abnormal Concentrations
Not Available
Associated Disorders and Diseases
Disease ReferencesNone
Associated OMIM IDsNone
DrugBank IDDB01268
Phenol Explorer Compound IDNot Available
FooDB IDNot Available
KNApSAcK IDNot Available
Chemspider ID4486264
KEGG Compound IDNot Available
BioCyc IDNot Available
BiGG IDNot Available
Wikipedia LinkSunitinib
METLIN IDNot Available
PubChem Compound5329102
PDB IDB49
ChEBI ID38940
Food Biomarker OntologyNot Available
VMH IDNot Available
MarkerDB IDNot Available
Good Scents IDNot Available
References
Synthesis ReferenceNot Available
Material Safety Data Sheet (MSDS)Not Available
General References
  1. Demetri GD, van Oosterom AT, Garrett CR, Blackstein ME, Shah MH, Verweij J, McArthur G, Judson IR, Heinrich MC, Morgan JA, Desai J, Fletcher CD, George S, Bello CL, Huang X, Baum CM, Casali PG: Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet. 2006 Oct 14;368(9544):1329-38. [PubMed:17046465 ]
  2. Motzer RJ, Hutson TE, Tomczak P, Michaelson MD, Bukowski RM, Rixe O, Oudard S, Negrier S, Szczylik C, Kim ST, Chen I, Bycott PW, Baum CM, Figlin RA: Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med. 2007 Jan 11;356(2):115-24. [PubMed:17215529 ]
  3. (). FDA label . .

Only showing the first 10 proteins. There are 15 proteins in total.

Enzymes

General function:
Involved in monooxygenase activity
Specific function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,8-cineole 2-exo-monooxygenase. The enzyme also hydroxylates etoposide.
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular weight:
57255.585
General function:
Involved in protein kinase activity
Specific function:
Receptor for VEGFC. Has a tyrosine-protein kinase activity
Gene Name:
FLT4
Uniprot ID:
P35916
Molecular weight:
145597.3
References
  1. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
  2. Deprimo SE, Bello CL, Smeraglia J, Baum CM, Spinella D, Rini BI, Michaelson MD, Motzer RJ: Circulating protein biomarkers of pharmacodynamic activity of sunitinib in patients with metastatic renal cell carcinoma: modulation of VEGF and VEGF-related proteins. J Transl Med. 2007 Jul 2;5:32. [PubMed:17605814 ]
  3. Katoh Y, Katoh M: Comparative integromics on VEGF family members. Int J Oncol. 2006 Jun;28(6):1585-9. [PubMed:16685460 ]
  4. Gridelli C, Maione P, Del Gaizo F, Colantuoni G, Guerriero C, Ferrara C, Nicolella D, Comunale D, De Vita A, Rossi A: Sorafenib and sunitinib in the treatment of advanced non-small cell lung cancer. Oncologist. 2007 Feb;12(2):191-200. [PubMed:17296815 ]
  5. Ahmed SI, Thomas AL, Steward WP: Vascular endothelial growth factor (VEGF) inhibition by small molecules. J Chemother. 2004 Nov;16 Suppl 4:59-63. [PubMed:15688612 ]
General function:
Involved in protein kinase activity
Specific function:
Receptor for the FL cytokine. Has a tyrosine-protein kinase activity
Gene Name:
FLT3
Uniprot ID:
P36888
Molecular weight:
112902.5
References
  1. O'Farrell AM, Abrams TJ, Yuen HA, Ngai TJ, Louie SG, Yee KW, Wong LM, Hong W, Lee LB, Town A, Smolich BD, Manning WC, Murray LJ, Heinrich MC, Cherrington JM: SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16. [PubMed:12531805 ]
  2. O'Farrell AM, Foran JM, Fiedler W, Serve H, Paquette RL, Cooper MA, Yuen HA, Louie SG, Kim H, Nicholas S, Heinrich MC, Berdel WE, Bello C, Jacobs M, Scigalla P, Manning WC, Kelsey S, Cherrington JM: An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients. Clin Cancer Res. 2003 Nov 15;9(15):5465-76. [PubMed:14654525 ]
  3. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  4. Schmidt-Arras D, Schwable J, Bohmer FD, Serve H: Flt3 receptor tyrosine kinase as a drug target in leukemia. Curr Pharm Des. 2004;10(16):1867-83. [PubMed:15180525 ]
  5. Yee KW, Schittenhelm M, O'Farrell AM, Town AR, McGreevey L, Bainbridge T, Cherrington JM, Heinrich MC: Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells. Blood. 2004 Dec 15;104(13):4202-9. Epub 2004 Aug 10. [PubMed:15304385 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
General function:
Involved in protein kinase activity
Specific function:
Receptor for VEGF or VEGFC. Has a tyrosine-protein kinase activity. The VEGF-kinase ligand/receptor signaling system plays a key role in vascular development and regulation of vascular permeability. In case of HIV-1 infection, the interaction with extracellular viral Tat protein seems to enhance angiogenesis in Kaposi's sarcoma lesions
Gene Name:
KDR
Uniprot ID:
P35968
Molecular weight:
151525.6
References
  1. Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM: In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. [PubMed:12538485 ]
  2. Schueneman AJ, Himmelfarb E, Geng L, Tan J, Donnelly E, Mendel D, McMahon G, Hallahan DE: SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models. Cancer Res. 2003 Jul 15;63(14):4009-16. [PubMed:12873999 ]
  3. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  4. Schoffski P, Dumez H, Clement P, Hoeben A, Prenen H, Wolter P, Joniau S, Roskams T, Van Poppel H: Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review. Ann Oncol. 2006 Aug;17(8):1185-96. Epub 2006 Jan 17. [PubMed:16418310 ]
  5. Amino N, Ideyama Y, Yamano M, Kuromitsu S, Tajinda K, Samizu K, Hisamichi H, Matsuhisa A, Shirasuna K, Kudoh M, Shibasaki M: YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors. Clin Cancer Res. 2006 Mar 1;12(5):1630-8. [PubMed:16533791 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
General function:
Involved in protein kinase activity
Specific function:
Protein tyrosine-kinase transmembrane receptor for CSF1 and IL34
Gene Name:
CSF1R
Uniprot ID:
P07333
Molecular weight:
107983.0
References
  1. Guo J, Marcotte PA, McCall JO, Dai Y, Pease LJ, Michaelides MR, Davidsen SK, Glaser KB: Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Mol Cancer Ther. 2006 Apr;5(4):1007-13. [PubMed:16648572 ]
  2. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
General function:
Involved in protein kinase activity
Specific function:
Receptor that binds both PDGFA and PDGFB and has a tyrosine-protein kinase activity
Gene Name:
PDGFRA
Uniprot ID:
P16234
Molecular weight:
122668.5
References
  1. Prenen H, Cools J, Mentens N, Folens C, Sciot R, Schoffski P, Van Oosterom A, Marynen P, Debiec-Rychter M: Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate. Clin Cancer Res. 2006 Apr 15;12(8):2622-7. [PubMed:16638875 ]
General function:
Involved in protein kinase activity
Specific function:
Receptor that binds specifically to PDGFB and PDGFD and has a tyrosine-protein kinase activity. Phosphorylates Tyr residues at the C-terminus of PTPN11 creating a binding site for the SH2 domain of GRB2
Gene Name:
PDGFRB
Uniprot ID:
P09619
Molecular weight:
123966.9
References
  1. Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM: In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. [PubMed:12538485 ]
  2. Abrams TJ, Lee LB, Murray LJ, Pryer NK, Cherrington JM: SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther. 2003 May;2(5):471-8. [PubMed:12748309 ]
  3. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  4. Pietras K, Hanahan D: A multitargeted, metronomic, and maximum-tolerated dose "chemo-switch" regimen is antiangiogenic, producing objective responses and survival benefit in a mouse model of cancer. J Clin Oncol. 2005 Feb 10;23(5):939-52. Epub 2004 Nov 22. [PubMed:15557593 ]
  5. Gollob JA: Sorafenib: scientific rationales for single-agent and combination therapy in clear-cell renal cell carcinoma. Clin Genitourin Cancer. 2005 Dec;4(3):167-74. [PubMed:16425993 ]
General function:
Involved in protein kinase activity
Specific function:
Receptor for VEGF, VEGFB and PGF. Has a tyrosine-protein kinase activity. The VEGF-kinase ligand/receptor signaling system plays a key role in vascular development and regulation of vascular permeability. Isoform SFlt1 may have an inhibitory role in angiogenesis
Gene Name:
FLT1
Uniprot ID:
P17948
Molecular weight:
150767.2
References
  1. O'Farrell AM, Foran JM, Fiedler W, Serve H, Paquette RL, Cooper MA, Yuen HA, Louie SG, Kim H, Nicholas S, Heinrich MC, Berdel WE, Bello C, Jacobs M, Scigalla P, Manning WC, Kelsey S, Cherrington JM: An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients. Clin Cancer Res. 2003 Nov 15;9(15):5465-76. [PubMed:14654525 ]
  2. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
General function:
Involved in protein kinase activity
Specific function:
This is the receptor for stem cell factor (mast cell growth factor). It has a tyrosine-protein kinase activity. Binding of the ligands leads to the autophosphorylation of KIT and its association with substrates such as phosphatidylinositol 3-kinase (Pi3K)
Gene Name:
KIT
Uniprot ID:
P10721
Molecular weight:
109863.7
References
  1. Abrams TJ, Lee LB, Murray LJ, Pryer NK, Cherrington JM: SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther. 2003 May;2(5):471-8. [PubMed:12748309 ]
  2. Schueneman AJ, Himmelfarb E, Geng L, Tan J, Donnelly E, Mendel D, McMahon G, Hallahan DE: SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models. Cancer Res. 2003 Jul 15;63(14):4009-16. [PubMed:12873999 ]
  3. Joensuu H: Second line therapies for the treatment of gastrointestinal stromal tumor. Curr Opin Oncol. 2007 Jul;19(4):353-8. [PubMed:17545799 ]
  4. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  5. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
General function:
Involved in monooxygenase activity
Specific function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular weight:
57108.065

Transporters

General function:
Involved in ATP binding
Specific function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular weight:
174205.6
References
  1. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]
General function:
Involved in ATP binding
Specific function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular weight:
141477.3
References
  1. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]
  2. Shukla S, Robey RW, Bates SE, Ambudkar SV: Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. doi: 10.1124/dmd.108.024612. Epub 2008 Oct 29. [PubMed:18971320 ]
General function:
Involved in ATP binding
Specific function:
Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from the brain. May be involved in brain-to-blood efflux. Appears to play a major role in the multidrug resistance phenotype of several cancer cell lines. When overexpressed, the transfected cells become resistant to mitoxantrone, daunorubicin and doxorubicin, display diminished intracellular accumulation of daunorubicin, and manifest an ATP- dependent increase in the efflux of rhodamine 123
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular weight:
72313.5
References
  1. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]
  2. Dai CL, Liang YJ, Wang YS, Tiwari AK, Yan YY, Wang F, Chen ZS, Tong XZ, Fu LW: Sensitization of ABCG2-overexpressing cells to conventional chemotherapeutic agent by sunitinib was associated with inhibiting the function of ABCG2. Cancer Lett. 2009 Jun 28;279(1):74-83. doi: 10.1016/j.canlet.2009.01.027. Epub 2009 Feb 18. [PubMed:19232821 ]
  3. Shukla S, Robey RW, Bates SE, Ambudkar SV: Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. doi: 10.1124/dmd.108.024612. Epub 2008 Oct 29. [PubMed:18971320 ]
General function:
Involved in ATP binding
Specific function:
May be an organic anion pump relevant to cellular detoxification
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular weight:
149525.3
References
  1. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]

Only showing the first 10 proteins. There are 15 proteins in total.