5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
Synonym(s):5-(2-(4-(2-Dimethylaminoethoxy)phenyl)-5-(4-pyridinyl)-1H-imidazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime
- CAS NO.:405554-55-4
- Empirical Formula: C27H27N5O2
- Molecular Weight: 453.54
- MDL number: MFCD16038645
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime?
The Uses of 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
SB 590885 is a potent Raf-B inhibitor.
What are the applications of Application
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.
Properties of 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
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 |
Safety information for 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention. |
Computed Descriptors for 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
InChIKey | MLSAQOINCGAULQ-QLTSDVKISA-N |
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