GW 5074|CAS 220904-83-6|DC Chemicals

Cas No.:	220904-83-6
Chemical Name:	5-Iodo-3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-2-indolinone
Synonyms:	2H-Indol-2-one,3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-1,3-dihydro-5-iodo-;GW5074;(3Z)-3-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-5-iodo-1H-indol-2-one;3-(3,5-Dibromo-4-hydroxybenzylidene)-5-iodo-1,3-dihydroindol-2-one;GW 5074 (GW-5074,GW5074);3-(3,5-Dibromo-4-hydroxybenzyliden)-5-iodo-1,3-dihydroindol-2-one;GW-5074;Raf1 Kinase Inhibitor I;STO521;Tocris-1381;GW 5074;B7W8RS1GG2;InSolution™ Raf1 Kinase Inhibitor I;5-Iodo-3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-2-indolinone;3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one;3-(3,5-dibromo-4-hydroxybenzylidene)-5-iodoindolin-2-one;(Z)-3-(3,5-Dibromo-4-hydroxybenzylidene)-5-iodoindolin-2-one;3-(3,5-Dibro
SMILES:	IC1C([H])=C([H])C2=C(C=1[H])/C(=C(\[H])/C1C([H])=C(C(=C(C=1[H])Br)O[H])Br)/C(N2[H])=O
Formula:	C₁₅H₈Br₂InO₂
M.Wt:	520.942
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.
In Vivo:	GW5074 (5 mg/Kg) completely prevents extensive bilateral striatal lesions induced by 3-NP in mice[1]. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice[2]. GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor[3].
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].

Cat. No.	Product name	Field of application
DC47985	GNE-9815	GNE-9815 is among the most highly kinase-selective RAF inhibitors targeting KRAS mutant cancers via combination treatment.
DC7719	ZM336372	ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc.
DC7307	TAK-632	TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR.
DC8791	Sorafenib free base (BAY-43-9006)	Sorafenib(BAY 43-9006) is a potent inhibitor of Raf-1 with IC50 values of 6 nM, 22 nM and 90 nM for Raf-1, B-Raf, and VEGFR2 respectively, BAY 43-9006 suppresses both wild-type and V599E mutant BRAF activity in vitro.
DC2098	Sorafenib (BAY-43-9006)	Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
DC7279	SB-590885	SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
DC9987	RAF709	RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
DC5049	RAF265 (CHIR-265)	RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.
DC9814	PLX7904(PB04)	PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.
DC6301	PLX-4720	PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

GW-5074