GW5074

(CAS No:220904-83-6)

GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.

CAS No:220904-83-6

Molecular Weight(MW):520.94

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	220904-83-6
Molecular formula(MF)	C₁₅H₈Br₂InO₂
Molecular Weight(MW):	520.94
Alias

Solubility

In vitro	DMSO	104 mg/mL (199.63 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo	30% propylene glycol, 5% Tween 80, 65% D5W	30 mg/mL

Biological Activity

Description

GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.

Targets

C-Raf ^[1]

9 nM

In vitro

GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types. ^[1]

In vivo

GW5074 is protective in an in vivo experimental model of Huntington’s disease. GW5074 (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. ^[1] GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor. ^[2] GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice. ^[3]