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Cat. No. Name Size Price Add Cart
KI3390SB590885QuoteQuote

Chemical Characteristic

Product NameSB590885
CAS No.405554-55-4
Molecular Weight 453.54
FormulaC27H27N5O2
Chemical NameN,N-dimethyl-2-[4-[(4Z)-4-(1-nitroso-2,3-dihydroinden-5-ylidene)-5-(1H-pyridin-4-ylidene)-1H-imidazol-2-yl]phenoxy]ethanamine
SmilesC\1(=N/O)/CCc2cc(ccc12)c1nc([nH]c1c1ccncc1)c1ccc(cc1)OCCN(C)C
Chemical Structure

Biological activities

SB-590885 is a novel, potent and selective inhibitor of the B-Raf kinase. SB-590885 preferentially inhibits growth of primary tumor cells containing B-RafV600E.[1] SB590885 potently inhibits V600EBRAF with an IC50 of 1 nM. SB590885 (100 to 300 nM) blocks ERK activity in V600EBRAF-expressing cells.[2] SB-590885 selectively inhibits Raf kinases with more potency towards B-Raf than c-Raf. SB-590885 potently inhibits the oncogenic B-Raf protein kinase with a Ki app of 0.16 nM. SB-590885 inhibits c-Raf with a Ki app of 1.72 nM. SB-590885 potently inhibits ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E. SB-590885 decreases tumorigenesis in murine xenografts in female nude mice established from mutant B-Raf-expressing A375P melanoma cells.[3]

Protocols

In vitro, SB590885 is dissolved in DMSO.[2]

References

[1] King AJ, et al. A novel, potent and selective small molecule inhibitor of B-Raf kinase, SB-590885, inhibits signal transduction and growth of cells bearing the B-Raf V600E mutation. Proc Amer Assoc Cancer Res. 2005, 46.
[2] Whittaker S, et al. Gatekeeper mutations mediate resistance to BRAF-targeted therapies. Sci Transl Med. 2010, 2(35): 35ra41.
[3] King AJ, et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res. 2006, 66(23): 11100-11105.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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