SB590885 is a potent and selective inhibitor of B-Raf kinase with Ki value of 0.16nM .
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 .
 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.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥4.54mg/mL in DMSO with gentle warming|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For 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.|
|Description||SB590885 is a potent inhibitor of B-Raf with a Ki value of 0.16 nM.|