3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide

3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide Basic information
Product Name:3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide
Synonyms:CENP-E inhibitor GS923295;CS-1336;GSK-923295;3-Chloro-N-((S)-1-(2-(dimethylamino)acetamido)-3-(4-(8-((S)-1-hydroxyethyl)-imidazo[1,2-a]pyri;3-chloro-N-((S)-1-(2-(diMethylaMiNA)acetaMido)-3-(4-(8-((R)-1-hydroxyethyl)iMidazo[1,2-a]pyridin-2-yl)phenyl)propan-2-yl)-4-isopropoxybenzaMide;3-Chloro-N-((S)-1-(2-(dimethylamino)acetamido)-3-(4-(8-((S)-1-hydroxyethyl)-imidazo[1,2-a]pyridin;Benzamide, 3-chloro-N-[(1S)-2-[[2-(dimethylamino)acetyl]amino]-1-[[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]methyl]ethyl]-4-(1-methylethoxy)-;3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide GSK-923295
CAS:1088965-37-0
MF:C32H38ClN5O4
MW:592.13
EINECS:256-495-9
Product Categories:Inhibitors
Mol File:1088965-37-0.mol
3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide Structure
3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide Chemical Properties
Melting point 197-198℃
density 1.25
storage temp. -20°C Freezer, Under inert atmosphere
solubility Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly, Sonicated)
form Solid
pka13.12±0.20(Predicted)
color Pale Yellow to Light Yellow
Safety Information
MSDS Information
3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide Usage And Synthesis
UsesGSK 923295 is the first potent, CENP-E-selective inhibitor that has been tested in Phase I clinical trials for treatment of Refractory Cancers.
Biological Activitygsk923295 is a specific inhibitor of cenp-e kinesin motor with ic50 value of 3.2 nm [1].centromere-associated protein e (cenp-e) is a mitotic kinesin, which is the connect of mitosis process with the mitotic checkpoint signaling. it interacts with spindle microtubules and contribute to the chromosome alignment, and thus it regulates the cell-cycle transition from metaphase to anaphase.when asynchronous cultured cells were exposed to gsk923295, the penetrant cell-cycle delay in mitosis was observed, which accompanied with morphological changes similar to rnai-mediated knockdown of cenp-e mrna. it indicated a significant inhibition of cenp-e by gsk923295. in the presence of gsk9232195, cenp-e microtubule (mt)-stimulated atpase showed a dramatic slowing of release of adp and pi, where the atp-bound form was stabilized and the activity of cenp-e was inhibited. this observation suggested gsk923295 inhibited cenp-e via the suppression of mt-stimulated atpase [1].in mouse model, mice bearing xenografts of the colo205 colon tumor cell line were administered with gsk923295 of 125 mg/kg. the result showed gsk923295-induced cell-cycle changes of tumor cells and increased scattered apoptosis body. additionally, long-term study via measuring tumor volume revealed significant antitumor activity of gsk923295, in a manner of dose-dependent [1].
storageStore at -20°C
references[1] wood k w et al. , antitumor activity of an allosteric inhibitor of centromere-associated protein-e. 2010, 107 (13): 5839-5844.
3-Chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl}-4-[(1-methylethyl)oxy]benzamide Preparation Products And Raw materials
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