GDC-0879

Reagent Authentication Certificate:

Chemical Probes Portal GDC-0879.pdf

Protein target name:

BRAF V600E

Mechanism of action:

ATP-competitive inhibitor

Recommended Concentration for use in cells:

1-300 nM

Probe Availability

Tocris (905281-76-7)

MedChem Express (905281-76-7)

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

TKL

HUGO ID:

HGNC:1097

Entrez gene ID:

673

UNIPROT ID:

P15056

Target alias:

B-RAF11, NS7, RAFB1, BRAF

Probe Details

Chemical Probes Portal ID:

CPP141

Probe alias:

905281-76-7, GDC0879, GDC 0879

PubChem CID:

11717001

ChEMBL ID:

CHEMBL525191

SMILES string:

C1C/C(=N\O)/C2=C1C=C(C=C2)C3=CN(N=C3C4=CC=NC=C4)CCO

InChi Key:

DEZZLWQELQORIU-RELWKKBWSA-N

PAINs evaluation:

PAINs free

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

63 nM

Potency assay:

In vitro substrate phosphorylation assay

Off target activity

Potency assay (off target):

1 uM GDC-0879 was tested against 140 kinases and exhibited >90% inhibitory activity against RAF kinases and >50% inhibitory activity against CSNK1D.

In cell validation

On target activity in cells

Target engagement assay (cells):

Indirect, in A375 cells, GDC-0879 led to comparable gene expression changes with an RNAi targeting BRAF.

In vivo validation

Organism:

CD1 mice

Dose:

25 mg/kg

Route of delivery:

Oral

Plasma half life:

3.8 h

Cmax:

5.5 ug/mL

Organ of Interest

Organ (O):

xenograft

Target engagement assay:

Indirect, assessment of substrate phosphorylation in xenograft tissue.

Primary Reference

Reference (doi):

10.1158/0008-5472.CAN-08-3563

Reference (PMID):

19276360

GDC-0879

Probe Availability

Probe Information

Target Details

B-RAF11, NS7, RAFB1, BRAF

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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GDC-0879

Probe Availability

Probe Information

Target Details

B-RAF11, NS7, RAFB1, BRAF

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?