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Biological Activity for SB 590885
SB 590885 is a 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.
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data for SB 590885
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 590885
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for SB 590885
The following data is based on the product molecular weight 453.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.1 mM||22.05 mL||110.24 mL||220.49 mL|
|0.5 mM||4.41 mL||22.05 mL||44.1 mL|
|1 mM||2.2 mL||11.02 mL||22.05 mL|
|5 mM||0.44 mL||2.2 mL||4.41 mL|
References for SB 590885
References are publications that support the biological activity of the product.
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 SB 590885, please let us know.
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Keywords: SB 590885, SB 590885 supplier, glaxosmithkline, SB590885, b-raf, braf, c-raf, kinases, inhibitors, inhibits, selective, Raf, Kinase, 2650, Tocris Bioscience
3 Citations for SB 590885
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
Balaburski et al (2013) A modified HSP70 inhibitor shows broad activity as an anticancer agent. Mol Cancer Res 11 219 PMID: 23303345
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
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Reviews for SB 590885
Average Rating: 5 (Based on 1 Review.)
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Endothelial cells were subjected to pre-treatment with 0.05 micromole SB 590885 prior to FGF2 treatment, isolated protein, and immunoblotted for pMEK1 levels.
Literature in this Area
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