SB 590885

Cat. No. 2650

SB 590885 C27H27N5O2 [405554-55-4]

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Chemical Name: 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime

Biological Activity

Potent B-Raf inhibitor (Kd = 0.3 nM). Selective for B-Raf against 46 other kinases (Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively). Decreases anchorage-independent growth of melanoma cell lines. Inhibits ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data

M.Wt:
453.54
Formula:
C27H27N5O2
Solubility:
Soluble to 10 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
405554-55-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

King et al (2006) Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res. 66 11100. PMID: 17145850.

Takle et al (2006) The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg.Med.Chem.Lett. 16 378. PMID: 16260133.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SB 590885 include:

Najm et al (2015) Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo. PLoS One 522 216. PMID: 25896324.

Wagenaar et al (2014) Resistance to vemurafenib resulting from a novel mutation in the BRAFV600E kinase domain. Pigment Cell Melanoma Res 27 124. PMID: 24112705.

Balaburski et al (2013) A modified HSP70 inhibitor shows broad activity as an anticancer agent. Mol Cancer Res 11 219. PMID: 23303345.

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Keywords: SB 590885, supplier, glaxosmithkline, SB590885, b-raf, braf, c-raf, kinases, inhibitors, inhibits, selective, Tocris Bioscience, Raf Kinase Inhibitor products

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