| Identification | Back Directory | [Name]
5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime | [CAS]
405554-55-4 | [Synonyms]
SB590885
GSK 2118436
SB-590885, >=98%
SB590885;SB-590885
SB590885(GSK2118436)
GSK 2118436(SB 590885)
(E)-5-(2-(4-(2-(Dimethylamino)ethoxy)phenyl)-5-(pyridin-4-yl)-1H-imidazol-4-yl)-2,3-dihydro-1H
5-[2-[4-[2-(DiMethylaMino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-iMidazol-4-yl]-2,3-dihydro-1H-inden-1-on
5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
(E)-5-(2-(4-(2-(dimethylamino)ethoxy)phenyl)-4-(pyridin-4-yl)-1H-imidazol-5-yl)-2,3-dihydroinden-1-one oxime
5-(2-(4-(2-(Dimethylamino)ethoxy)phenyl)-5-(pyridin-4-yl)-1H-imidazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime
1H-Inden-1-one, 5-[2-[4-[2-(diMethylaMino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-iMidazol-4-yl]-2,3-dihydro-, oxiMe
(E)-5-(2-(4-(2-(dimethylamino)ethoxy)phenyl)-5-(pyridin-4-yl)-1H-imidazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime
5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime USP/EP/BP | [Molecular Formula]
C27H27N5O2 | [MDL Number]
MFCD16038645 | [MOL File]
405554-55-4.mol | [Molecular Weight]
453.54 |
| Chemical Properties | Back Directory | [density ]
1.27 | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble2mg/mL (clear solution, warmed) | [form ]
powder | [color ]
white to beige | [InChIKey]
MLSAQOINCGAULQ-QLTSDVKISA-N |
| Hazard Information | Back Directory | [Uses]
Selective for B-Raf against 46 other kinases. SB 590885 dihydrochloride decreases anchorage-independent growth of melanoma cell lines. Inhibits ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E. | [Definition]
ChEBI: (E)-SB-590885 is an N-{5-[2-{4-[2-(dimethylamino)ethoxy]phenyl}-4-(pyridin-4-yl)-1H-imidazol-5-yl]-2,3-dihydro-1H-inden-1-ylidene}hydroxylamine in which the oxime group has E configuration. | [Biological Activity]
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]. | [in vivo]
Administration of SB-590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth[1]. | [IC 50]
B-Raf: 0.16 nM (Ki); c-Raf: 1.72 nM (Ki) | [storage]
Store at -20°C | [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. |
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