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SB590885

In stock
Catalog No.
B1406
Potent B-Raf inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$150.00
In stock
10mg
$120.00
In stock
50mg
$480.00
In stock
100mg
$780.00
In stock
250mg
$1,380.00
In stock

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SB590885 is a potent and selective inhibitor of B-Raf kinase with Ki value of 0.16nM [1].

SB590885 is a potent inhibitor of oncogenic B-Raf protein kinase with Ki value of 0.16nM. It is more potent to inhibit B-Raf than C-Raf. The Ki value of SB590885 for C-Raf is 1.72nM. SB590885 is a quite selective inhibitor. It shows no activity against 48 other human kinases such as Abl, AMPK, CK1, CK2 and ERK2. It is found that SB590885 binds to B-Raf within the ATP-binding pocket and stabilizes the active conformation of B-Raf. SB590885 decreases the phosphorylation of ERK and shows anti-proliferation only in tumor cells expressing oncogenic B-Raf V600E. The normal cells and tumor cells not expressing mutant B-Raf have no sensitivity towards SB590885 except the normal melanocytes and primary melanoma cells expressing wild-type B-Raf. Moreover, SB590885 is also found to decrease the transformed and tumorigenic properties of malignant cells expressing mutant B-Raf [1].

References:
[1] King A J, Patrick D R, Batorsky R S, et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer research, 2006, 66(23): 11100-11105.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt453.55
Cas No.405554-55-4
FormulaC27H27N5O2
Solubility≥4.54mg/mL in DMSO with gentle warming
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
SDFDownload SDF
Canonical SMILESCN(C)CCOC1=CC=C(C=C1)C2=NC(=C3C=CC4=C(CCC4=C3)N=O)C(=C5C=CNC=C5)N2
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description SB590885 is a potent inhibitor of B-Raf with a Ki value of 0.16 nM.
Targets B-Raf          
IC50 0.16 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

SB590885