GDC-0879

Description

Biological Activity

Protocol(Only for Reference)

Chemical Information

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Customer Reviews (4)

Animal Study: ^[2]

References

貨號 Cat. No.: S1104
規格 Size: 5~200mg
品牌 Brand: Selleckchem

GDC-0879

Catalog No.S1104

4 Reviews 8 Product Citations

GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well; no inhibition known to other protein kinases.

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10mM/1mLIn DMSO	USD 415	In stock	0 1 2 3 4 5 6 7 8 9 10
2mg	USD 138	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 214	In stock	0 1 2 3 4 5 6 7 8 9 10
10mg	USD 340	In stock	0 1 2 3 4 5 6 7 8 9 10
25mg	USD 592	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Animal Models	Female nu/nu mice
Dosages	100 mg/kg
Administration	Oral gavage
Solubility	0.5% methylcellulose/0.2% Tween 80, 30 mg/mL

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Molecular Weight (MW)	334.37
Formula	C₁₉H₁₈N₄O₂
CAS No.	905281-76-7

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	67 mg/mL (200 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	5 mg/mL (14 mM)
	In vivo	0.5% methylcellulose/0.2% Tween 80,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * 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 Name	(E)-5-(1-(2-hydroxyethyl)-3-(pyridin-4-yl)-1H-pyrazol-4-yl)-2,3-dihydroinden-1-one oxime

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.33437	3.3437	6.6874	10.0311

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Description

GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well; no inhibition known to other protein kinases.

0.13 nM ^[1]

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]

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]

Click to enlarge	Rating
	Source	J Natl Cancer Inst, 2012, 104(21), 1673-9. GDC-0879 purchased from Selleck
	Method	Western Blot
	Cell Lines	primary human melanocytes
	Concentrations	1 uM
	Incubation Time	18 h
	Results	Furthermore, in BRAFV600E melanoma cells, the highly selective BRAFV600E inhibitor GDC-0879 and three selective MEK inhibitors [PD184352/CI-1040, U0126, PD98059] did not suppress c-Jun levels, although they effectively reduced phospho-ERK levels.