tivozanib   Click here for help

GtoPdb Ligand ID: 6058

Synonyms: AV-951 | AV951 | Fotivda® | KRN-951 | KRN951 | VEGFR tyrosine kinase inhibitor IV
Approved drug PDB Ligand
tivozanib is an approved drug (EMA (2017), FDA (2021))
Compound class: Synthetic organic
Comment: Tivozanib is an oral VEGF receptor tyrosine kinase inhibitor.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 8
Topological polar surface area 107.74
Molecular weight 454.1
XLogP 3.53
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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Canonical SMILES COc1cc2c(ccnc2cc1OC)Oc1ccc(c(c1)Cl)NC(=O)Nc1noc(c1)C
Isomeric SMILES COc1cc2c(ccnc2cc1OC)Oc1ccc(c(c1)Cl)NC(=O)Nc1noc(c1)C
InChI InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28)
InChI Key SPMVMDHWKHCIDT-UHFFFAOYSA-N

Large-scale screening data

EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1-2

Key to terms and symbols Click column headers to sort
Target Name in screen Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
ABL proto-oncogene 1, non-receptor tyrosine kinase Abl/ABL1 Hs Inhibitor Inhibition -6.0 -7.0
EPH receptor A2 EphA2/EPHA2 Hs Inhibitor Inhibition -3.0 -3.0
EPH receptor B2 EphB2/EPHB2 Hs Inhibitor Inhibition -2.0 -1.0
ABL proto-oncogene 2, non-receptor tyrosine kinase Arg/ABL2(ARG) Hs Inhibitor Inhibition -2.0 -1.0
LCK proto-oncogene, Src family tyrosine kinase Lck activated Hs Inhibitor Inhibition -2.0 1.0
fms related receptor tyrosine kinase 4 Flt4/FLT4 Hs Inhibitor Inhibition -1.0 -1.0
LYN proto-oncogene, Src family tyrosine kinase Lyn/LYN Hs Inhibitor Inhibition -1.0 2.0
Raf-1 proto-oncogene, serine/threonine kinase c-RAF/RAF1 Hs Inhibitor Inhibition 0.0 1.0
colony stimulating factor 1 receptor Fms/FMS Hs Inhibitor Inhibition 0.0 0.0
fms related receptor tyrosine kinase 1 Flt1/FLT1(VEGFR1) Hs Inhibitor Inhibition 0.0 -1.0
Displaying the top 10 targets  View all targets in screen »