Name: GDC-0879
Brand: Selleck Chemicals
SKU: S1104
Rating: 5 (43 reviews)

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Quality Control

Batch: Purity: 99.84%

99.84

Related Targets	ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Other Raf Inhibitors	LY3009120 Exarafenib (KIN-2787) Avutometinib (Ro5126766, CH5126766) PLX-4720 AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265) PLX8394 (Plixorafenib, FORE8394)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
human MALME3M cells	Function assay	Inhibition of ERK1/2 phosphorylation in human MALME3M cells, IC50=0.063 μM
human A375 cells	Proliferation assay	Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50=0.5 μM
human A375 cells	Function assay	Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50=1 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	334.37	Formula	C₁₉H₁₈N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	905281-76-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AR-00341677			Smiles	C1CC(=NO)C2=C1C=C(C=C2)C3=CN(N=C3C4=CC=NC=C4)CCO

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (197.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% methylcellulose 1 0.2% Tween 80 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (29.91mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose+0.2% Tween 80 clear solution, and mix evenly to make it a uniform suspension. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	B-Raf (A375, Colo205 cells) 0.13 nM
In vitro	GDC-0879 also inhibits cellular pERK with IC50 of 63 nM. This compound 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. It potently inhibits B-Raf^V600E in Malme3M cells with IC50 of 0.75 μM. This chemical also shows EC50 values < 0.5 μM in many tumour cells (A375, 624, SK-MEL-28, Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34, and Colo201).
In vivo	In GDC-0879 treated mice, both cell line- and patient-derived BRAFV600E tumours exhibit stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared to mutant KRAS-expressing tumours. Although there is involvement of activated RAF signalling in RAS-induced tumorigenesis, decreased time to progression is observed for some KRAS-mutant tumours following this compound administration. Whereas this chemical-mediated efficacy is associated strictly with B-Raf^V600E status, MEK inhibition also attenuates proliferation and tumour growth of cell lines expressing wild-type BRAF (81% KRAS mutant, 38% KRAS wild type). The responsiveness of B-Raf^V600E melanoma cells to this agent could be dramatically altered by pharmacologic and genetic modulation of PI3K pathway activity.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19147858/ [2] https://pubmed.ncbi.nlm.nih.gov/19276360/

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GDC-0879 B-Raf Inhibitor

Chemical Structure

Molecular Weight: 334.37