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SB-743921 hydrochloride

产品编号 T2255Cas号 940929-33-9
别名 SB743921 HCl, SB743921

SB-743921 hydrochloride (SB743921 HCl) 是一种有效的驱动蛋白纺锤体蛋白 KSP 抑制剂,Ki 值为 0.1 nM。

SB-743921 hydrochloride

SB-743921 hydrochloride

纯度: ≥95%
产品编号 T2255 别名 SB743921 HCl, SB743921Cas号 940929-33-9

SB-743921 hydrochloride (SB743921 HCl) 是一种有效的驱动蛋白纺锤体蛋白 KSP 抑制剂,Ki 值为 0.1 nM。

规格价格库存数量
2 mg¥ 623现货
5 mg¥ 947现货
10 mg¥ 1,680现货
25 mg¥ 2,870现货
50 mg¥ 4,170现货
100 mg¥ 5,930现货
200 mg¥ 7,990现货
1 mL x 10 mM (in DMSO)¥ 1,190现货
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"SB-743921 hydrochloride"的相关化合物库

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纯度:≥95%
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产品介绍

生物活性
产品描述
SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).
靶点活性
KSP:0.1 nM(Ki)
体外活性
对于多种异种移植人的肿瘤,如Colo205,MCF-7, SK-MES, H69, OVCAR-3HT-29, MX-1, MDA-MB-231, A2780,SB-743921均能产生明显的抑制效应,抑制细胞生长的活性.
体内活性
SB 743921阻断了有丝分裂纺锤体的产生,因此能将细胞在有丝分裂期积累并产生细胞坏死,对于人的KSP(Ki=0.1 nM)和鼠的KSP(Ki=0.12 nM)。
激酶实验
Biochemistry assay: The motor domains of KSP (amino acids 1–360) is expressed as in Escherichia coli BL21(DE3) as COOH-terminal 6-his fusion proteins. Bacterial pellets are lysed in a microfluidizer with a lysis buffer [50 mM Tris-HCl; 50 mM KCl, 10 mM imidazole, 2 mM MgCl2, 8 mM β-mercaptoethanol, 0.1 mM ATP (pH 7.4)], and proteins are purified using Ni-NTA agarose affinity chromatography, with an elution buffer consisting of 50 mM PIPES, 10% sucrose, 300 mM imidazole, 50 mM KCl, 2 mM MgCl2, mM β-mercaptoethanol, and 0.1 mM ATP (pH 6.8). Steady-state measurements of ATPase activity are performed with a pyruvate kinase–lactate dehydrogenase detection system that coupled the appearance of ADP with oxidation of NADH. Absorbance changes are monitored at 340 nm. All biochemical experiments are performed in PEM25 buffer [25 mM Pipes/KOH (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM SB 743921 for experiments involving microtubules. Rates of ADP release are measured in a stopped-flow apparatus; the decrease in fluorescence of MANT-ATP is monitored. Rates of Pi release are measured in a stopped-flow apparatus, using bacterial phosphate binding protein modified with 7-diethylamino-3-((((2 maleimidyl)ethyl)amino)carbonyl)coumarin (MDCC) dye. Ki estimates of KSP inhibitors are extracted from the dose–response curves, with explicit correction for enzyme concentration. Tubulin polymerization by measuring changes in absorbance at 340 nm is monitored. The assay is performed in 100-μL volumes in 96-well half-area microtiter plates, using a microplate reader with the incubation temperature set at 37 °C.
细胞实验
All cells including HeLa cells are cultured in 10% FCS in RPMI 1640 in 5% CO2. We assessed 48-hour growth inhibition by serial dilution of SB 743921 relative to DMSO-treated cells in 96-well microtiter plates, using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium. Cell growth is represented as the ratio of absorbance of treated cells to DMSO control, plotted by concentration and fitted to a four-parameter curve. Concentrations at which cellular growth is inhibited by 50% are extrapolated from the curve fit. The DNA content of HeLa cells cultured in the presence or absence of 1 μM SB 743921 for 24 hours is assessed by propidium iodide staining and flow cytometry. Immunofluorescence images are collected of HeLa cells treated for 24 hours with 1 μM SB 743921, fixed with 2% formaldehyde, permeabilized, and stained with DM1-α, anti-γ-tubulin, and 1 μg/mL 4′,6-diamidino-2-phenylindole, and with Alexa 488 secondary goat antirabbit IgG and Rhodamine-X goat antimouse IgG. Images are collected with a DeltaVision Restoration Microscopy System at a magnification of ×600. Z stacks (0.2 μm) are collected, and out of focus information is removed by constrained iterative deconvolution. Z stacks are then compressed into to a single image plane. (Only for Reference)
别名SB743921 HCl, SB743921
化学信息
分子量553.52
分子式C31H34Cl2N2O3
CAS No.940929-33-9
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 60 mg/mL (108.4 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.8066 mL9.0331 mL18.0662 mL90.3310 mL
5 mM0.3613 mL1.8066 mL3.6132 mL18.0662 mL
10 mM0.1807 mL0.9033 mL1.8066 mL9.0331 mL
20 mM0.0903 mL0.4517 mL0.9033 mL4.5165 mL
50 mM0.0361 mL0.1807 mL0.3613 mL1.8066 mL
100 mM0.0181 mL0.0903 mL0.1807 mL0.9033 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
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μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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