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| | 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime Basic information |
| | 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime Chemical Properties |
| density | 1.27 | | storage temp. | Sealed in dry,Store in freezer, under -20°C | | solubility | DMSO: soluble2mg/mL (clear solution, warmed) | | form | powder | | color | white to beige | | InChIKey | MLSAQOINCGAULQ-QLTSDVKISA-N |
| WGK Germany | 3 | | HS Code | 2933998090 |
| | 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime Usage And Synthesis |
| Uses | SB 590885 is a potent Raf-B inhibitor. | | 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]. | | 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. |
| | 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime Preparation Products And Raw materials |
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