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Cabozantinib | Cabozantinib : ATP Competitive inhibitor of KDR
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KDR
  • IC50:0.035 nM
  • IC50:6.7 nM
  • IC50:4.1-7.7 nM
  • IC50:31 nM
  • IC50:9 nM
ATP Competitive
up to 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - c-Met 1.3 nM, Ret 4 nM, Kit 4.6 nM, Flt-1/3/4 12 nM/11.3 nM/6 nM, Tie2 14.3 nM, AXL 7 nM

Potency Assay Off-Target:
AlphaScreen Assay, Coupled Luciferase Assay, Radiometric Assay
Selectivity Assessment Description:
The inhibition profile of cabozantinib against a broad panel of 270 human kinases was determined ...

Potency
Cellular
In Vitro

KDR

Mode of Action: ATP Competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1535-7163.MCT-11-0264

In Vivo Validations

Mouse
Dose: 100 mg/Kg
Route of delivery: Oral

DOI Reference: 10.1158/1535-7163.MCT-11-0264

Orthogonal Probes def

BRIVANIB

Chemical Information

Molecular Formula C28H24FN3O5
SMILEs COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC
InChI InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
Molecular weight 501.17 Da
AlogP 5.5408
HBond acceptors 8
HBond donors 2
Atoms 61

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

No SERP comments found for Cabozantinib

Probe Cabozantinib is in the process of SERP review.

Please continue to check back for new reviews and commentary.