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GDC-0879

Name: GDC-0879
Brand: Selleck Chemicals
SKU: S1104
Rating: 5 (36 reviews)

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.

CAS No. 905281-76-7

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

Purity & Quality Control

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Raf Signaling Pathway Map

Biological Activity

Description

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-Raf^V600E mutant, with IC50 of 59 nM and 29 nM for pMEK1 inhibition respectively. GDC-0879 potently inhibits B-Raf^V600E 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=>

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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-Raf^V600E 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-Raf^V600E 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

References

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. Click to purchase: Tween 80	30 mg/mL

Chemical Information

Molecular Weight	334.37
Formula	C₁₉H₁₈N₄O₂
CAS No.	905281-76-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CC(=NO)C2=C1C=C(C=C2)C3=CN(N=C3C4=CC=NC=C4)CCO

Download GDC-0879 SDF

In vivo Formulation Calculator (Clear solution)

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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

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Handling Instructions

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