GDC-0879

Name: GDC-0879
Brand: Selleck Chemicals
SKU: S1104
Rating: 5 (31 reviews)

For research use only.

Catalog No.S1104 Synonyms: AR-00341677

31 publications

Molecular Weight(MW): 334.37

GDC-0879 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.

Selleck's GDC-0879 has been cited by 31 publications

Cancer Cell, 2016, 12;30(3):485-498

PubMed: 27523909 ( click the link to review the publication )

Cancer Discov, 2013, 3(3):350-62

PubMed: 23288408 ( click the link to review the publication )

Cell Syst, 2020, 10(3):240-253

PubMed: 32191874 ( click the link to review the publication )

Hum Cell, 2019, 10.1007/s13577-019-00270-4

PubMed: 31586300 ( click the link to review the publication )

Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520

PubMed: 31618797 ( click the link to review the publication )

Sci Adv, 2019, 5(8):eaav8463

PubMed: 31453322 ( click the link to review the publication )

Exp Gerontol, 2019, 126:110691

PubMed: 31421186 ( click the link to review the publication )

Cell Death Differ, 2019, 10.1038/s41418-019-0416-4

PubMed: 31541179 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(4):806-813

PubMed: 29167314 ( click the link to review the publication )

ACS Med Chem Lett, 2018, 9(12):1199-1204

PubMed: 30613326 ( click the link to review the publication )

Cell Signal, 2018, 44:127-137

PubMed: 29329780 ( click the link to review the publication )

Small GTPases, 2018, 10.1080/21541248.2018.1446697

PubMed: 29634387 ( click the link to review the publication )

Med Oncol, 2017, 35(1):7

PubMed: 29214525 ( click the link to review the publication )

Nat Commun, 2016, 7:13781

PubMed: 28000790 ( click the link to review the publication )

Elife, 2016, 10.7554/eLife.09976

PubMed: 26882073 ( click the link to review the publication )

PLoS One, 2016, 11(2):e0147538

PubMed: 26828720 ( click the link to review the publication )

Stem Cell Reports, 2016, 7(3):355-369

PubMed: 27569062 ( click the link to review the publication )

Nat Struct Mol Biol, 2015, 22(1):37-43

PubMed: 25437913 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1278

PubMed: 24901049 ( click the link to review the publication )

Cell Microbiol, 2014, 16(9):1441-55

PubMed: 24779413 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2013, 110(35):E3281-90

PubMed: 23918355 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2013, 27(1):124-33

PubMed: 24112705 ( click the link to review the publication )

Int J Oncol, 2013, 44(3):959-69

PubMed: 24366069 ( click the link to review the publication )

PLoS One, 2013, 8(2):e56134

PubMed: 23418523 ( click the link to review the publication )
J Biomol Screen, 2013, 19(4):526-37

PubMed: 24361645 ( click the link to review the publication )

J Natl Cancer Inst, 2012, 104(21):1673-9

PubMed: 22997239 ( click the link to review the publication )

Cell Death Differ, 2012, 19(12):2029-39

PubMed: 22858545 ( click the link to review the publication )

Sci Signal, 2012, 5(224):rs4

PubMed: 22589389 ( click the link to review the publication )

Mol Cell Proteomics, 2012, 11(6):M112.017764

PubMed: 22345495 ( click the link to review the publication )

P Natl Acad Sci USA, 2011, 108(15):6067-72

PubMed: 21441104 ( click the link to review the publication )

PLoS One, 2011, 6(8):e23235

PubMed: 21829721 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Raf Inhibitors

Biological Activity

Description

GDC-0879 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-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	Activity Description	PMID
human MALME3M cells	MVvGeY5kfGmxbjDhd5NigQ>?	MnTyTY5pcWKrdHnvckBw\iCHUluxM\|IheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJG1CVE2HM12gZ4VtdHNuIFnDOVA:OC5yNkOg{txO	MoO1NVE4OTdyMEG=
human A375 cells	NYXHVodkWHKxbHnm[ZJifGmxbjDhd5NigQ>?	MlPjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDM{e1JINmdGy\|IHX4dJJme3OrbnegRk1T[WZiVk[wNGUhdXW2YX70JIFv\CC5aXzkJJR6eGViUnHzMEBKSzVyPUCuOUDPxE1?	MY[yNlgxQDlzMR?=
human A375 cells	NVz2VZQ1TnWwY4Tpc44h[XO\|YYm=	M1XzOmlvcGmkaYTpc44hd2ZiYj3SZYYhcW5iaIXtZY4hSTN5NTDj[YxteyCjc4Pld5Nm\CCyaH;zdIhwenmuYYTpc44hd2ZiRWLLMEBKSzVyPUGg{txO	NES2[JMzOjhyOEmxNS=>

... Click to View More Cell Line Experimental Data

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

Animal Research:^[2]	- Collapse Animal Models: Female nu/nu mice Dosages: 100 mg/kg Administration: Oral gavage (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	66 mg/mL warmed (197.38 mM)
	Ethanol	5 mg/mL (14.95 mM)
	Water	Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download GDC-0879 SDF

Molecular Weight	334.37
Formula	C₁₉H₁₈N₄O₂
CAS No.	905281-76-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	AR-00341677
Smiles	OCC[N]1C=C(C2=CC=C\3C(=C2)CCC3=N\O)C(=N1)C4=CC=NC=C4

In vivo Formulation Calculator (Clear solution)

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

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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.

Bio Calculators

Molarity Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Computed Result

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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

Tel: +1-832-582-8158 Ext:3

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Raf Signaling Pathway Map

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GDC-0879