Molecular Formula | C32H38ClN5O4 |
Molar Mass | 592.13 |
Density | 1.25 |
Melting Point | 197-198℃ |
Solubility | Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly, Sonicated) |
Appearance | Solid |
Color | Pale Yellow to Light Yellow |
pKa | 13.12±0.20(Predicted) |
Storage Condition | -20°C Freezer, Under inert atmosphere |
In vitro study | GSK923295 was the first potent, selective inhibitor of mitotic kinesin centromere-associated protein-E(CENP-E). GSK923295 non-competitively inhibits CENP-E MT-stimulated ATPase activity with ATP and microtubules (MT), and has a K I of 3.2 nM, which is more selective than other kinesins. GSK923295 inhibited the release of inorganic phosphorus, stabilized CENP-E of the Mada domain interacting with microtubules, and reduced the ATP-promoted CENP-E decomposition rate from MT(koff, MT) by more than 50-fold. GSK923295 leads to metaphase chromosomal arrangement failure, inducing mitotic arrest. GSK923295 effectively inhibited the growth of 237 tumor cell lines, with an average GI50 of 253 nM and a median GI50 of 32 nM. When mitogen-activated protein kinase (MEK/ERK) signaling was also inhibited, GSK923295 was more effective in suppressing tumor cell growth. |
In vivo study | GSK923295 treatment of tumors resulted in a significant increase in mitosis and free apoptotic bodies. GSK923295 resulted in an increase in the proportion of 4n to 2n nuclei in a dose-dependent manner. GSK923295 at a dose of 125 mg/kg treatment of Colo205 transplanted tumor, has a strong anti-tumor activity, this effect is dose dependent. GSK923295 has significant anti-tumor activity in solid tumor models, including Ewing sarcoma, rod-shaped tumor, and rhabdomyosarcoma xenografts, which may be a valuable therapeutic target in pediatric cancer. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.689 ml | 8.444 ml | 16.888 ml |
5 mM | 0.338 ml | 1.689 ml | 3.378 ml |
10 mM | 0.169 ml | 0.844 ml | 1.689 ml |
5 mM | 0.034 ml | 0.169 ml | 0.338 ml |