Chemical Probes logo
TIVOZANIB | TIVOZANIB : Inhibitor of VEGFR1-3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FLT1
  • IC50:30.6 nM
  • IC50:0.21 nM
KDR
  • IC50:6.5 nM
  • IC50:0.16 nM
FLT4
  • IC50:15 nM
  • IC50:0.24 nM
Inhibitor
10 nM and no more than 50 nM.
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Activity-based assay at 1 µM ATP (ProQinase). KRN951 also inhibited c-Kit and PDGFR-β phosphorylatio ...

Potency
Cellular
In Vitro

FLT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-05-4290

KDR

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-05-4290

FLT4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-05-4290

In Vivo Validations

Rat
Dose: 0.04 mg/Kg
Route of delivery: Oral
Plasma half life: 9.25 h
Systemic clearance: 122 mL/h/Kg
Cmax: 21.6 ng/mL
Tmax: 3.63 h
Area Under the Curve:: 0.34 ug*h/mL
Volume of Distribution at Steady-State: 1634 ml/Kg

DOI Reference: 10.1158/0008-5472.CAN-05-4290

Dose: 0.2 mg/Kg
Route of delivery: Oral
Plasma half life: 7.78 h
Systemic clearance: 124 mL/h/Kg
Cmax: 108 ng/mL
Tmax: 2.63 h
Area Under the Curve:: 1.64 ug*h/mL
Volume of Distribution at Steady-State: 1399 mL/Kg

DOI Reference: 10.1158/0008-5472.CAN-05-4290

Dose: 1 mg/Kg
Route of delivery: Oral
Plasma half life: 8.13 h
Systemic clearance: 132 mL/h/Kg
Cmax: 484 ng/mL
Tmax: 4.25 h
Area Under the Curve:: 7.64 ug*h/mL
Volume of Distribution at Steady-State: 1543 mL/Kg

DOI Reference: 10.1158/0008-5472.CAN-05-4290

Dose: 5 mg/mL
Route of delivery: Oral
Plasma half life: 7.94 h
Systemic clearance: 113 mL/h/Kg
Cmax: 2823 ng/mL
Tmax: 3.50 h
Area Under the Curve:: 44.5 ug*h/mL
Volume of Distribution at Steady-State: 1293 mL/Kg

DOI Reference: 10.1158/0008-5472.CAN-05-4290

Chemical Information

Molecular Formula C22H19ClN4O5
SMILEs COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC
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)
Molecular weight 454.10 Da
AlogP 0.0
HBond acceptors 9
HBond donors 2
Atoms 51

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 21 Aug 2023 )
Cellular Use Rating
In Model Organisms
Tivozanib is a clinically approved VEGF kinase inhibitor with established efficacy and suitable safety in renal cell carcinoma. I has therefore been extensively profiled in vivo across multiple species...
by SERP
(on 15 Feb 2024 )
Cellular Use Rating
In Model Organisms
Cellular IC50s are cited as being sub-nanomolar to single-digit-nanomolar. Given that cited biochemical selectivity over other RTK targets is only 10-100-fold, cellular concentrations should be kept as...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria