SB 590885

Pricing Availability Delivery Time Qty
Cat.No. 2650 - SB 590885 | C27H27N5O2 | CAS No. 405554-55-4
Description: Potent B-Raf inhibitor
Chemical Name: 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Literature

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
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 405554-55-4
PubChem ID 11316960
InChI Key DPCXEUSDRQOOGZ-QLYXXIJNSA-N
Smiles CN(C)CCOC(C=C4)=CC=C4C1=NC(C3=CC=C(C(CC5)=NO)C5=C3)=C(C2=CC=NC=C2)N1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 4.54 10
ethanol 2.27 5mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 453.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.2 mL 11.02 mL 22.05 mL
5 mM 0.44 mL 2.2 mL 4.41 mL
10 mM 0.22 mL 1.1 mL 2.2 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: glaxosmithkline SB590885 b-raf braf c-raf kinases inhibitors inhibits selective Raf Kinase

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

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


Do you know of a great paper that uses SB 590885 from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
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A collection of over 190 products for immunology research, the guide includes research tools for the study of:

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for SB 590885

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