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| 品牌 | absin | CAS | 1088965-37-0 |
|---|---|---|---|
| 分子式 | C32H38ClN5O4 | 纯度 | ＞98% |
| 分子量 | 592.13 | 货号 | abs810313 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a first-in-class, specific allosteri | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
GSK-923295 1088965-37-0
| 产品描述 | |
| 描述 | GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. Phase 1. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | GSK-923295,GSK923295 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO 100 mg/mL (168.88 mM) Ethanol 100 mg/mL (168.88 mM) |
| 生物活性 | |
| 靶点 | CENP-E |
| In vitro(体外研究) | GSK923295 is the first potent and selective inhibitor of the mitotic kinesin centromere-associated protein-E (CENP-E). GSK923295 is uncompetitive with both ATP and microtubules (MT), inhibiting CENP-E MT-stimulated ATPase activity with a Ki of 3.2 nM, highly selective over other kinesins. GSK923295 inhibits release of inorganic phosphate and stabilizes CENP-E motor domain interaction with microtubules, reduces the rate of ATP-promoted dissociation of CENP-E from MT (koff, MT) by more than 50-fold. GSK923295 causes failure of metaphase chromosome alignment and induces mitotic arrest. GSK923295 is a potent inhibitor of tumor cell growth, with an average GI50 of 253 nM and a median GI50 of 32 nM for 237 tumor cell lines. GSK923295 inhibits tumor cell growth more effectively when mitogen-activated protein kinase (MEK/ERK) signaling is also inhibited. |
| In vivo(体内研究) | GSK923295 produces clear increases in the abundance of mitotic figures and scattered apoptotic bodies in tumors. GSK923295 causes a dose-dependent increase in the ratio of 4n to 2n nuclei. GSK923295 exhibits robust, dose-dependent antitumor activity against Colo205 xenografts, including partial and complete regressions at the 125 mg/kg dose. GSK923295 demonstrates significant antitumor activity against solid tumor models, inducing CRs in Ewing sarcoma, rhabdoid, and rhabdomyosarcoma xenografts, may be a valuable therapeutic target in pediatric cancer. |
| 研究领域 | |
| 研究领域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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