GDC-0879

Name: GDC-0879
Brand: Selleck Chemicals
SKU: S1104
Rating: 5 (30 reviews)

For research use only. Not for use in humans.

Catalog No.S1104 Synonyms: AR-00341677

30 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 30 publications

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

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

Sci Adv, 2019, 5(8):eaav8463

PubMed: 31453322 ( 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 )

Exp Gerontol, 2019, 126:110691

PubMed: 31421186 ( 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 )

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 )

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

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

PLoS One, 2016, 11(2):e0147538

PubMed: 26828720 ( 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 )

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

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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	Mn\CSpVv[3Srb36gZZN{[Xl?	NEHGZ5BKdmirYnn0bY9vKG:oIFXST\|EwOiCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hVUGOTVWzUUBk\WyuczygTWM2OD1yLkC2N{DPxE1?	NVK4[ZQ5OTF5MUewNFE>
human A375 cells	MXfQdo9tcW[ncnH0bY9vKGG\|c3H5	MmXZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDM{e1JINmdGy\|IHX4dJJme3OrbnegRk1T[WZiVk[wNGUhdXW2YX70JIFv\CC5aXzkJJR6eGViUnHzMEBKSzVyPUCuOUDPxE1?	NV3aOFRROjJ6MEi5NVE>
human A375 cells	M3K2b2Z2dmO2aX;uJIF{e2G7	NVfvPI9rUW6qaXLpeIlwdiCxZjDiMXJi\iCrbjDoeY1idiCDM{e1JINmdGy\|IHHzd4V{e2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFVmstKEmFNUC9NUDPxE1?	M{f0UlIzQDB6OUGx

... 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 Formulation: 0.5% methylcellulose/0.2% Tween 80 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
Storage	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

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Raf Signaling Pathway Map

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