A potent inhibitor of B-Raf (Kd = 0.3 nM) that less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases; blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations

SB-590885 – 5 mg

Brand:
Cayman
CAS:
405554-55-4
Storage:
-20
UN-No:
Non-Hazardous - /

B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} SB-590885 is a potent inhibitor of B-Raf (Kd = 0.3 nM).{27151} It less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases.{27151,27149} SB-590885 blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations.{27149,27150} Melanoma cells expressing the B-RafV600E mutation can drive invasion through alternative pathways in the presence of SB-590885, suggesting that combination therapy is needed to completely block cell invasion.{27150} SB-590885 has also been used to study the role of B-Raf in cerebral ischemia.{27152}  

 

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Description

A potent inhibitor of B-Raf (Kd = 0.3 nM) that less effectively inhibits c-Raf (Ki = 1.72 nM) and has little effect at 46 other kinases; blocks activation of ERK1/2 and anchorage-independent cell proliferation of melanoma cells with either wild type or V600E B-Raf at nanomolar concentrations

Formal name: 5-[2-[4-[2-(dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime

Synonyms: 

Molecular weight: 453.5

CAS: 405554-55-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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