GDC-0879

Catalog No.S1104 Synonyms: AR-00341677

For research use only.

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

CAS No. 905281-76-7

Selleck's GDC-0879 has been cited by 36 publications

Purity & Quality Control

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MALME3M cells M1OwbGZ2dmO2aX;uJIF{e2G7 Ml\3TY5pcWKrdHnvckBw\iCHUluxM|IheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1CVE2HM12gZ4VtdHNuIFnDOVA:OC5yNkOg{txO M4LZNVEyPzF5MECx
human A375 cells Mmf1VJJwdGmoZYLheIlwdiCjc4PhfS=> MojORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHX4dJJme3OrbnegRk1T[WZiVk[wNGUhdXW2YX70JIFv\CC5aXzkJJR6eGViUnHzMEBKSzVyPUCuOUDPxE1? MXGyNlgxQDlzMR?=
human A375 cells NFjhXVFHfW6ldHnvckBie3OjeR?= NH\KeVdKdmirYnn0bY9vKG:oIHKtVoFnKGmwIHj1cYFvKEF|N{WgZ4VtdHNiYYPz[ZN{\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXST{whUUN3ME2xJO69VQ>? NFrrZlgzOjhyOEmxNS=>
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]

Protocol (from reference)

Animal Research:[2]
  • Animal Models: Female nu/nu mice
  • Dosages: 100 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 334.37
Formula

C19H18N4O2

CAS No. 905281-76-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(=NO)C2=C1C=C(C=C2)C3=CN(N=C3C4=CC=NC=C4)CCO

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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