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Brivanib | Brivanib : ATP competitive inhibitor of KDR
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KDR
  • IC50:26 nM
  • Ki:25 nM
  • IC50:40 nM
  • IC50:276 nM
ATP competitive
1 µM
up to 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - FLK1 89 nM, FGFR1 148 nM

Selectivity Assessment Description:
Kinase Selectivity IC50 (nM): VEGFR-1 380, FGFR-1 148, PDGFR-β >6000, EGFR >1900, LCK >2 ...

Potency
Cellular
In Vitro

KDR

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm051106d

In Vivo Validations

Mouse, Rat
Dose: 10, 60, 90 Mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 2.7 (IV), 3.6 (PO) h
Systemic clearance: 9.3 (IV) mL/min/kg

DOI Reference: 10.1021/jm051106d

Orthogonal Probes def

CABOZANTINIB

Chemical Information

Molecular Formula C19H19FN4O3
SMILEs Cc1cc2c(F)c(Oc3ncnn4cc(OC[C@@H](C)O)c(C)c34)ccc2[nH]1
InChI InChI=1S/C19H19FN4O3/c1-10-6-13-14(23-10)4-5-15(17(13)20)27-19-18-12(3)16(26-8-11(2)25)7-24(18)22-9-21-19/h4-7,9,11,23,25H,8H2,1-3H3/t11-/m1/s1
Molecular weight 370.14 Da
AlogP 3.518440000000002
HBond acceptors 7
HBond donors 2
Atoms 46

References

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Expert Reviews

by SERP
(on 19 Oct 2025 )
Cellular Use Rating
In Model Organisms
Brivanib (BMS-540215) is a potent ATP-competitive inhibitor of KDR (VEGFR2) kinase. Due to limited selectivity data (only KDR plus seven additional kinases were tested), additional data would be necessary...
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