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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

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

References

Publications

Cross References

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 comments )
by SERP
(on 12 Dec 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
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