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GDC-0879 | GDC-0879 : ATP competitive inhibitor of BRAF
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
BRAF (Mutant:V600E)
  • IC50:63 nM
ATP competitive
1-300 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
1 uM GDC-0879 was tested against 140 kinases and exhibited >90% inhibitory activity against RAF kina ...
Selectivity Assessment Description:
1 uM GDC-0879 was tested against 140 kinases and exhibited >90% inhibitory activity against RAF kina ...

Potency
Cellular
In Vitro

BRAF (Mutant:V600E)

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

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

In Vivo Validations

Mouse
Dose: 25 mg/kg
Route of delivery: Oral
Plasma half life: 3.8 h
Organ of interest (O): xenograft
Target engagement assay: Indirect, assessment of substrate phosphorylation in xenograft tissue.

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

Chemical Information

Molecular Formula C19H18N4O2
SMILEs OCCn1cc(-c2ccc3c(c2)CC/C3=N\O)c(-c2ccncc2)n1
InChI InChI=1S/C19H18N4O2/c24-10-9-23-12-17(19(21-23)13-5-7-20-8-6-13)15-1-3-16-14(11-15)2-4-18(16)22-25/h1,3,5-8,11-12,24-25H,2,4,9-10H2/b22-18+
Molecular weight 334.14 Da
AlogP 2.7289000000000003
HBond acceptors 6
HBond donors 2
Atoms 43

Vendors

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Expert Reviews

by SERP
(on 3 Jun 2016)
Cellular Use Rating
In Model Organisms
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...
by SERP
(on 21 Nov 2016)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 12 Dec 2016)
Cellular Use Rating
(The reviewer did not leave any public comments)
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria