GDC-0879

ATP-competitive inhibitor of BRAF (Mutant:V600E)

Structure

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In Cells

(3 ratings)

In Model Organisms

(2 ratings)

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Information

Protein target names: BRAF (Mutant:V600E)

Mechanism of action: ATP-competitive inhibitor

Recommended in-cell concentration:

1-300 nM

Primary References:

Secondary References:

DOI - 10.1016/j.ccr.2014.07.007

Probe Availability:

In Vitro Validations

Uniprot ID: P15056

Target Class: Kinase

Target SubClass: TKL

Potency: IC50

Potency Value: 63 nM

Potency Assay: In vitro substrate phosphorylation assay

PDB ID for probe-target interaction (3D structure): 4MNF

Target aliases:

Serine/threonine-protein kinase B-raf, RAFB1, BRAF ...

DOI Reference: 10.1158/0008-5472.CAN-08-3563

In Cell Validations

In Vivo Data

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SERP ratings and comments

SERP Ratings

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In Model Organisms

SERP Comments:

The chemotype for this probe is very selective for RAF but is expected to inhibit both mutant and wild-type forms as well as c-RAF. The fact that it is orally bioavailable makes it a very useful probe to interrogate RAF biology.

(last updated: 3 Jun 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 21 Nov 2016 )

SERP Ratings

In Cell Rating

(last updated: 12 Dec 2016 )