ChemicalBook > Product Catalog >Biochemical Engineering >Inhibitors >Mitogen-activated protein kinase (MAPK) >Raf inhibitors >5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-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

5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime Suppliers list
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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
Product Name:5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime
Synonyms:5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-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;GSK 2118436(SB 590885);SB590885(GSK2118436);5-[2-[4-[2-(DiMethylaMino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-iMidazol-4-yl]-2,3-dihydro-1H-inden-1-on;(E)-5-(2-(4-(2-(dimethylamino)ethoxy)phenyl)-4-(pyridin-4-yl)-1H-imidazol-5-yl)-2,3-dihydroinden-1-one oxime;GSK 2118436;SB-590885, >=98%
CAS:405554-55-4
MF:C27H27N5O2
MW:453.54
EINECS:
Product Categories:Inhibitors;Potent B-Raf inhibitor.;MAPK
Mol File:405554-55-4.mol
5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime Structure
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
InChIKeyMLSAQOINCGAULQ-QLTSDVKISA-N
SMILESCN(C)CCOc1ccc(cc1)-c2nc(-c3ccc4c(CC\C4=N\O)c3)c([nH]2)-c5ccncc5
Safety Information
WGK Germany 3
HS Code 2933998090
Storage Class11 - Combustible Solids
MSDS Information
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
UsesSB 590885 is a potent Raf-B inhibitor.
DefinitionChEBI: (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 Activitysb590885 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 50B-Raf: 0.16 nM (Ki); c-Raf: 1.72 nM (Ki)
storageStore 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
Tag:5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime(405554-55-4) Related Product Information
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