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CAS 1088965-37-0 GSK-923295 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 GSK-923295 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

Name:GSK-923295 CAS:1088965-37-0 MF:C32H38ClN5O4 MW:592.13 Purity:96% Package:100g;1kg;10kg; Made in China Worldwide Delivery

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Product introduction

Introduction and application of CAS 1088965-37-0 GSK-923295 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;

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)-;

Specification:

ITEMS	SPECIFICATION
CAS	1088965-37-0
MF	C32H38ClN5O4
MW	592.13
Melting point	197-198℃
Boiling point	403.2±20.0 °C(Predicted)
Density	1.25
Acidity coefficient	13.12±0.20(Predicted)
Color	Light yellow to pale yellow
Form	Solid
Storage condition	-20°C Freezer, Under inert atmosphere

Use:

Scientific research synthesis

GSK923295 is the first potent, selective inhibitor of the mitotic kinesin centromere-associated protein-E (CENP-E). GSK923295 inhibits ATPase activity stimulated by CENP-E MTs non-competitively with ATP and microtubules (MTs) with a Ki of 3.2 nM, which is highly selective over other kinesins. GSK923295 inhibits inorganic phosphate release, stabilizes the interaction of the CENP-E motor domain with microtubules, and reduces the rate of ATP-promoted dissociation of CENP-E from MTs (koff, MTs) by more than 50-fold. GSK923295 causes metaphase chromosome alignment failure and induces mitotic arrest. GSK923295 effectively inhibits tumor cell growth in 237 tumor cell lines with an average GI50 of 253 nM and a median GI50 of 32 nM. GSK923295 is more effective in inhibiting tumor cell growth when mitogen-activated protein kinase (MEK/ERK) signaling is also inhibited.

GSK923295 treatment of tumors significantly increased mitosis and free apoptotic bodies. GSK923295 caused an increase in the ratio of 4n to 2n nuclei in a dose-dependent manner. GSK923295 treated Colo205 transplanted tumors at a dose of 125 mg/kg and had strong anti-tumor activity in a dose-dependent manner. GSK923295 has significant anti-tumor activity in solid tumor models, including Ewing sarcoma, rod tumors, and rhabdomyosarcoma xenografts, which may be a valuable therapeutic target in pediatric cancers.

Package and transportation:Normal

Package:100g;1kg;10kg;