Golvatinib

Protein target name:

MET, KDR

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

up to 5 uM

Probe Availability

MedChemExpress

Selleck Chemicals

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

HUGO ID:

HGNC:7029 HGNC:6307

Entrez gene ID:

4233 3791

UNIPROT ID:

P08581 P35968

Target alias:

MET proto-oncogene, receptor tyrosine kinase, AUTS9, DFNB97, HGFR, RCCP2, c-Met, kinase insert domain receptor, KDR, CD309, FLK1, VEGFR, VEGFR2

Probe Details

Chemical Probes Portal ID:

CPP1237

Probe alias:

E-7050; E7050

PubChem CID:

16118392

ChEMBL ID:

CHEMBL3039525

SMILES string:

O=C(NC1=CC=C(C=C1F)OC2=CC(NC(N3CCC(CC3)N4CCN(CC4)C)=O)=NC=C2)C5(CC5)C(NC6=CC=C(C=C6)F)=O

InChi Key:

UQRCJCNVNUFYDX-UHFFFAOYSA-N

Orthogonal probe:

abozantinib

Validation in Cells and Model Organisms

In cell validation

On target activity in cells

Potency in cells:

IC50

14 nM MET, 16 nM KDR, 24 nM in SNU-5, 23 nM in Hs746T, 6.2 nM in EBC-1, 37 nM in MKN45

Potency assay (cells):

C-Met Autophosphorylation Inhibition, VEGF-induced phosphorylation assays, Cell Proliferation assay (SNU-5, Hs746T, EBC-1, and MKN45 tumor cells)

In vivo validation

Organism:

Mouse

Dose:

50-200 mg/Kg

Route of delivery:

Oral

Primary Reference

Reference (doi):

10.1111/j.1349-7006.2009.01343.x

Reference (PMID):

19832844

Golvatinib

Probe Availability

Probe Information

Target Details

MET proto-oncogene, receptor tyrosine kinase, AUTS9, DFNB97, HGFR, RCCP2, c-Met, kinase insert domain receptor, KDR, CD309, FLK1, VEGFR, VEGFR2

Probe Details

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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Golvatinib

Probe Availability

Probe Information

Target Details

MET proto-oncogene, receptor tyrosine kinase, AUTS9, DFNB97, HGFR, RCCP2, c-Met, kinase insert domain receptor, KDR, CD309, FLK1, VEGFR, VEGFR2

Probe Details

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?