| Identification | Back Directory | [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 | [CAS]
1088965-37-0 | [Synonyms]
CS-1336
GSK-923295
GSK-923295;GSK923295
CENP-E inhibitor GS923295
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-(dimethylamino)acetamido)-3-(4-(8-((S)-1-hydroxyethyl)-imidazo[1,2-a]pyridin
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-[(2S)-1-[[2-(dimethylamino)acetyl]amino]-3-[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]propan-2-yl]-4-propan-2-yloxybenzamide
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
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 ISO 9001：2015 REACH
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 | [EINECS(EC#)]
256-495-9 | [Molecular Formula]
C32H38ClN5O4 | [MDL Number]
MFCD16038931 | [MOL File]
1088965-37-0.mol | [Molecular Weight]
592.13 |
| Chemical Properties | Back Directory | [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 | [pka]
13.12±0.20(Predicted) | [color ]
Pale Yellow to Light Yellow |
| Hazard Information | Back Directory | [Uses]
GSK 923295 is the first potent, CENP-E-selective inhibitor that has been tested in Phase I clinical trials for treatment of Refractory Cancers. | [Biological Activity]
gsk923295 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]. | [in vivo]
Xenografts of mice treated with GSK-923295 (GSK923295) shows significant tumor growth delay compared to the control arm (NB-EBc1 p<0.0001; NB-1643 p=0.018; NB-1691 p=0.0018)[3]. | [IC 50]
CENP-E: 1.6 nM (Ki, Canine CENP-E) | [storage]
Store 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. |
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| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Telephone: |
020-13556033878 2965585218 13556033878 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList15061/0_EN.htm |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
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