Cabozantinib

Protein target name:

KDR

Mechanism of action:

Inhibitor, ATP Competitive

Recommended Concentration for use in cells:

up to 10 uM

Probe Availability

MedChemExpress

TOCRIS

Selleck Chemicals

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

HUGO ID:

HGNC:6307

Entrez gene ID:

3791

UNIPROT ID:

P35968

Target alias:

Kinase insert domain receptor, CD309, FLK1, VEGFR, VEGFR2

Probe Details

Chemical Probes Portal ID:

CPP1204

Probe alias:

XL184; XL-184; Cometriq; BMS-907351

PubChem CID:

25102847

ChEMBL ID:

CHEMBL2105717

SMILES string:

O=C(C1(CC1)C(NC2=CC=C(F)C=C2)=O)NC3=CC=C(C=C3)OC4=C5C=C(OC)C(OC)=CC5=NC=C4

InChi Key:

ONIQOQHATWINJY-UHFFFAOYSA-N

Orthogonal probe:

Brivanib

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

0.035 nM

Potency assay:

AlphaScreen Assay

Off target activity

Potency (off target):

IC50

Off target protein and potency:

c-Met 1.3 nMRet 4 nMKit 4.6 nMFlt-1/3/4 12 nM/11.3 nM/6 nMTie2 14.3 nMAXL 7 nM

Potency assay (off target):

AlphaScreen Assay, Coupled Luciferase Assay, Radiometric Assay

Probe Selectivity in Vitro:

The inhibition profile of cabozantinib against a broad panel of 270 human kinases was determined using luciferase-coupled chemiluminescence 33P-phosphoryl transfer, or AlphaScreen technology. Cabozantinib is also a MET (Met Mutants) inhibitor with IC50s in the range of 1-15 nM.

In cell validation

On target activity in cells

Potency in cells:

IC50

6.7 nM

Potency assay (cells):

Phosphorylation Inhibition Assay

In vivo validation

Organism:

Mouse

Dose:

100 mg/Kg

Route of delivery:

Oral

Primary Reference

Reference (doi):

10.1158/1535-7163.MCT-11-0264

Reference (PMID):

21926191

Cabozantinib

Probe Availability

Probe Information

Target Details

Kinase insert domain receptor, CD309, FLK1, VEGFR, VEGFR2

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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Cabozantinib

Probe Availability

Probe Information

Target Details

Kinase insert domain receptor, CD309, FLK1, VEGFR, VEGFR2

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?