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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Cytoskeleton > GSK-923295CAS：1088965-37-0
Molecular Formula：C32H38ClN5O4
Molecular Weight：592.13
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 1088965-37-0 |
| Name | GSK-923295 |
| Molecular Formula | C32H38ClN5O4 |
| Molecular Weight | 592.13 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 256-495-9 |
| MDL | MFCD16038931 |
| SMILES | O=C(N[C@@H](CC1=CC=C(C2=CN3C(C([C@@H](O)C)=CC=C3)=N2)C=C1)CNC(CN(C)C)=O)C4=CC(Cl)=C(C=C4)OC(C)C |
| Target Point | Kinesin |
| Passage | Cytoskeleton |
| Background | GSK923295 is an allosteric inhibitor of the primary specific allosteric inhibitor CENP-E kinesin ATPase. |
| Biological Activity | GSK-923295 是一种特异性的变构 CENP-E 驱动蛋白 ATPase 活性抑制剂，作用于人类和犬类此酶，Ki 分别为 3.2±0.2 nM 和 1.6±0.1 nM[1-3]。 |
| In Vitro | GSK923295是一种有效的选择性人类CENPE小分子抑制剂，Ki为3.2 nM。 GSK923295对一组19种人神经母细胞瘤细胞系具有广泛的疗效，平均生长IC50为41 nM [3]。GSK923295与ATP和MT无竞争性，抑制CENP-E MT刺激的ATP酶活性，人和犬的Ki分别为3.2±0.2 nM和1.6±0.1 nM。 GSK923295抑制无机磷酸盐的释放并稳定CENP-E运动结构域与微管的相互作用[1]。 GSK923295在一组237个癌细胞系中具有广泛的生长抑制活性，并且在11个小鼠异种移植肿瘤模型中的8个中产生显著的肿瘤生长延迟，对于SW48，RKO，IC50分别为17.2nM，55.6nM，42nM和51.9nM(BRAF突变体)，SW620(KRAS突变体)和HCT116(KRAS突变体)，分别为[2]。 |
| In Vivo | 与对照组相比，用GSK-923295处理的小鼠的异种移植物显示出显著的肿瘤生长延迟(NB-EBc1 p <0.0001; NB-1643 p = 0.018; NB-1691 p = 0.0018)[3]。 |
| Cell Experiment | 接种后24小时(T0)和暴露于不同浓度的GSK-923295(0.01 nM，0.1 nM，1 nM，10 nM，100 nM，1μM，10μM和100μM)后测定DNA含量72小时(T72)。所有T72测量值归一化为T0。使用XLfit曲线拟合工具分析曲线以确定GSK923295的浓度，相对于T0和Ymax值(GI50)产生50％的生长抑制[1]。 |
| Animal Experiment | 小鼠[3] CB17 scid小鼠用于繁殖皮下植入的神经母细胞瘤肿瘤。使用卡尺测量肿瘤直径。计算肿瘤体积。一旦肿瘤体积超过200 mm3，将小鼠随机分组(每组10只)，接受GSK923295 125 mg/kg IP或载体(96％酸化水，2％DMAC，2％CREM)，总共6剂，使用3天，4天休息，3天疗程。 |
| Data Literature Source | [1]. Wood KW，et al. Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. [2]. Mayes PA，et al. Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E (CENP-E) inhibition. Int J Cancer. 2013 Feb 1;132(3):E149-57. [3]. Balamuth NJ，et al. Serial transcriptome analysis and cross-species integration identifies centromere-associated protein E as a novel neuroblastoma target. Cancer Res. 2010 Apr 1;70(7):2749-58 |
| Unit | Bottle |
| Specification | 2mg 5mg |
GSK923295是一级特异性变构抑制剂CENP-E驱动蛋白ATPase的变构抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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