Home MAPK Raf inhibitor GDC-0879 For research use only.

GDC-0879

Synonyms: AR-00341677

GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.

GDC-0879 Chemical Structure

GDC-0879 Chemical Structure

CAS No. 905281-76-7

Purity & Quality Control

GDC-0879 Related Products

Signaling Pathway

Raf Signaling Pathways

Raf Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MALME3M cells Function assay Inhibition of ERK1/2 phosphorylation in human MALME3M cells, IC50=0.063 μM 11717001
human A375 cells Proliferation assay Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50=0.5 μM 22808911
human A375 cells Function assay Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50=1 μM 22808911
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Biological Activity

Description GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.
Targets
B-Raf [1]
(A375, Colo205 cells)
0.13 nM
In vitro
In vitro GDC-0879 also inhibits cellular pERK with IC50 of 63 nM. GDC-0879 shows comparable potency in A375 melanoma and Colo205 colorectal carcinoma cell lines, both of which are B-RafV600E mutant, with IC50 of 59 nM and 29 nM for pMEK1 inhibition respectively. GDC-0879 potently inhibits B-RafV600E in Malme3M cells with IC50 of 0.75 μM. GDC-0879 also shows EC50 values < 0.5 μM in many tumor cells (A375, 624, SK-MEL-28, Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34, and Colo201). [1]
In Vivo
In vivo In GDC-0879 treated mice, both cell line- and patient-derived BRAFV600E tumors exhibit stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared to mutant KRAS-expressing tumors. Although there is involvement of activated RAF signaling in RAS-induced tumorigenesis, decreased time to progression is observed for some KRAS-mutant tumors following GDC-0879 administration. Whereas GDC-0879-mediated efficacy is associated strictly with B-RafV600E status, MEK inhibition also attenuates proliferation and tumor growth of cell lines expressing wild-type BRAF (81% KRAS mutant, 38% KRAS wild type). The responsiveness of B-RafV600E melanoma cells to GDC-0879 could be dramatically altered by pharmacologic and genetic modulation of PI3K pathway activity. [2]
Animal Research Animal Models Female nu/nu mice
Dosages 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 334.37 Formula

C19H18N4O2
CAS No. 905281-76-7 SDF Download GDC-0879 SDF
Smiles C1CC(=NO)C2=C1C=C(C=C2)C3=CN(N=C3C4=CC=NC=C4)CCO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (197.38 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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