Description
SB590885(GSK2118436) can inhibit B-raf, B-Raf(V600E), and c-Raf with IC50 of 3.2 nM, 0.8 nM, and 5.0 nM.
Storage
2 years at -20 centigrade
Targets
B-raf, B-Raf(V600E), c-Raf
Molecular Formula
C27H27N5O2
Chemical Name
(E)-5-(2-(4-(2-(dimethylamino)ethoxy)phenyl)-4-(pyridin-4-yl)-1H-imidazol-5-yl)-2,3-dihydroinden-1-one oxime
Solubility
DSMO 5 mg/mL Water
In vitro
GSK2118436 is a novel, potent, and selective Raf kinase inhibitor that is capable of inhibiting the kinase activity of wild-type B-Raf, B-RafV600E and c-Raf with IC50 values of 3.2, 0.8, and 5.0 nM, respectively. Kinase panel screening for over 270 kinases has indicated thatthis inhibitor is selective for Raf kinase, with 400 fold selectivitytowards B-Raf over 91% of the other kinases tested. Specificcellular inhibition of B-RafV600E kinase by this inhibitor leadsto decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle, followedby cell death. This inhibition is selective for cancer cellsthat specifically encode the mutation for B-Raf V600E.
In vivo
Oral compoundadministration inhibits the growth of B-RafV600E mutant melanoma(A375P) and colon cancer (Colo205) human tumor xenografts, growingsubcutaneously in immuno-compromised mice.
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