Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK923295 是一种特异性的变构着丝粒相关蛋白-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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 433 | 现货 | ||
2 mg | ¥ 626 | 现货 | ||
5 mg | ¥ 917 | 现货 | ||
10 mg | ¥ 1,550 | 现货 | ||
25 mg | ¥ 3,190 | 现货 | ||
50 mg | ¥ 4,730 | 现货 | ||
100 mg | ¥ 6,760 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,290 | 现货 |
产品描述 | GSK923295 is a selective allosteric inhibitor of CENP-E kinesin motor ATPase(Ki=3.2 nM). |
靶点活性 | CENP-E:3.2 nM(Ki) |
体外活性 | 在多种实体瘤模型中,如尤因肉瘤,杆状瘤,横纹肌肉瘤移植瘤,GSK923295均能产生显著地抗肿瘤活性.Colo205移植瘤中,GSK923295(125 mg/kg)能够抑制肿瘤生长,使核分裂和游离的凋亡小体明显增加. |
体内活性 | 在癌细胞系中,GSK923295具有广谱抗肿瘤活性,对于 SW48(IC50=17.2 nM), RKO (BRAF mutant)( IC50=55.6 nM), SW620 (KRAS mutant)(IC50=42 nM), and HCT116 (KRAS mutant)(IC50=51.9 nM)。在人类神经母细胞瘤细胞系中,GSK923295平均生长IC50为41 nM。 |
激酶实验 | Enzymology: Kinesin motor domains are expressed in Escherichia coli BL21(DE3) and purified. CENP-E proteins includes residues 2–340 with a carboxyl-terminal 6-his tag. All studies using MT are conducted in PEM25 buffer [25 mM PipesK+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM paclitaxel. The IC50 for steady-state inhibition is determined at 500 μM ATP, 5 μM MT, and 1 nM CENP-E in PEM25 buffer. |
细胞实验 | Cell-growth inhibition assays are performed by MDS in 384-well plates, and DNA content of fixed cells stained with DAPI using an Incell 1000 is analyzed. DNA content is determined 24 h after seeding (T0) and after exposure to varying concentrations of drug for an additional 72 h (T72). All T72 measurements are normalized to T0. Curves are analyzed using the XLfit curve-fitting tool to determine the concentration of GSK923295 yielding 50% growth inhibition relative to T0 and Ymax values (GI50).(Only for Reference) |
分子量 | 592.13 |
分子式 | C32H38ClN5O4 |
CAS No. | 1088965-37-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 93 mg/mL (157.1 mM)
DMSO: 93 mg/mL (157.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.6888 mL | 8.4441 mL | 16.8882 mL | 42.2205 mL |
5 mM | 0.3378 mL | 1.6888 mL | 3.3776 mL | 8.4441 mL | |
10 mM | 0.1689 mL | 0.8444 mL | 1.6888 mL | 4.222 mL | |
20 mM | 0.0844 mL | 0.4222 mL | 0.8444 mL | 2.111 mL | |
50 mM | 0.0338 mL | 0.1689 mL | 0.3378 mL | 0.8444 mL | |
100 mM | 0.0169 mL | 0.0844 mL | 0.1689 mL | 0.4222 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK-923295 1088965-37-0 Apoptosis Cytoskeletal Signaling Kinesin GSK923295 inhibit Inhibitor GSK 923295 inhibitor