Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ispinesib (SB-715992) 是一种选择性可逆的驱动蛋白纺锤体蛋白抑制剂,具有抗肿瘤特性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 247 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 695 | 现货 | ||
10 mg | ¥ 1,160 | 现货 | ||
25 mg | ¥ 2,180 | 现货 | ||
50 mg | ¥ 3,560 | 现货 | ||
100 mg | ¥ 5,890 | 现货 | ||
500 mg | ¥ 11,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 789 | 现货 |
产品描述 | Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties. |
靶点活性 | KSP (HsEg5):1.7 nM(Ki app) |
体外活性 | 携带移植瘤的小鼠模型, Ispinesib(4.5-15 mg/kg)能够抑制Colo205, Colo201, HT-29细胞生长.在小鼠实体瘤中,用Ispinesib处理(6 -10 mg/kg ),Madison 109肺癌, M5076肉瘤,及L1210和P388白血病能够被抑制.携带乳腺癌细胞MCF-7, HCC1954, MDA-MB-468,和KPL4移植瘤的小鼠中,Ispinesib(8-10 mg/kg )抑制肿瘤生长. |
体内活性 | 在PC-3前列腺癌细胞中, Ispinesib(5 nM 和 30 nM)通过调节信号的基因表达水平,抑制细胞增殖和诱导细胞凋亡。在乳腺癌细胞系中, Ispinesib(7.4 nM–600 nM)具有广谱抑制活性。在肿瘤细胞系中(Colo205, Colo201, HT-29, M5076, Madison-109,和MX-1),Ispinesib(IC50=1.2-9.5 nM) 具有很强细胞毒性。 |
激酶实验 | Steady-State Kinetic Analysis of Human KSP ATPase Activity and Inhibition by Ispinesib: Kinesin specificity analysis is carried out using a pyruvate kinase-lactate dehydrogenase detection system that couples the production of ADP to oxidation of NADH. Absorbance changes are monitored at 340 nm. Steady-state studies using nanomolar concentrations of KSP are performed using a sensitive fluorescence-based assay utilizing a pyruvate kinase, pyruvate oxidase, and horseradish peroxidase (HRP) coupled detection system that couples the generation of ADP to oxidation of Amplex Red to fluorescent resorufin. Generation of resorufin is monitored by fluorescence (λexcitation = 520 nm and λemission = 580 nm). Steady-state biochemical experiments are performed in PEM25 buffer [25 mM Pipes-K+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM paclitaxel for experiments involving microtubules. The IC50 for steady-state inhibition is determined at 500 μM ATP, 5 μM Microtubules, and 1 nM KSP in PEM25 buffer. Ki app (apparent inhibitor dissociation constant) values of Ispinesib are extracted from the dose-response curves, with explicit correction for enzyme concentration by using the Morrison equation. Inhibitor modality (e.g., competitive, noncompetitive, uncompetitive, or mixed) under steady-state conditions is determined by measuring the effect of inhibitor concentration on initial velocity as a function of substrate concentrations. Data are fit using equations in GraFit to velocity equations for the various modes of inhibition. |
细胞实验 | Cells are plated in log phase of growth in 96-well plates and treated with Ispinesib for 72 hours. Then, cell growth is measured using CellTiter-Glo, and luminescence is detected using BioTek FLx800. Data are analyzed and the IC50 value, defined as the drug concentration that results in 50% growth inhibition relative to control, is calculated.(Only for Reference) |
别名 | 伊匹尼塞, 伊斯平斯, CK0238273, SB-715992 |
分子量 | 517.06 |
分子式 | C30H33ClN4O2 |
CAS No. | 336113-53-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 95 mg/mL (183.7 mM)
DMSO: 95 mg/mL (183.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.934 mL | 9.6701 mL | 19.3401 mL | 48.3503 mL |
5 mM | 0.3868 mL | 1.934 mL | 3.868 mL | 9.6701 mL | |
10 mM | 0.1934 mL | 0.967 mL | 1.934 mL | 4.835 mL | |
20 mM | 0.0967 mL | 0.4835 mL | 0.967 mL | 2.4175 mL | |
50 mM | 0.0387 mL | 0.1934 mL | 0.3868 mL | 0.967 mL | |
100 mM | 0.0193 mL | 0.0967 mL | 0.1934 mL | 0.4835 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。
Ispinesib 336113-53-2 Apoptosis Cell Cycle/Checkpoint Cytoskeletal Signaling Kinesin KSP CK-0238273 伊匹尼塞 inhibit SB715992 Inhibitor 伊斯平斯 CK0238273 CK 0238273 SB 715992 SB-715992 inhibitor