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Dinaciclib

产品编号 T1912Cas号 779353-01-4
别名 SCH 727965, PS-095760

Dinaciclib (SCH 727965) 是一种 CDK 抑制剂,抑制 CDK1、CDK2、CDK5 和 CDK9 (IC50=3/1/1/4 nM),具有选择性。Dinaciclib 具有潜在的抗肿瘤活性,可以抑制胸甘 (dThd) DNA 的整合。

Dinaciclib
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Dinaciclib

纯度: 99.75%
产品编号 T1912 别名 SCH 727965, PS-095760Cas号 779353-01-4

Dinaciclib (SCH 727965) 是一种 CDK 抑制剂,抑制 CDK1、CDK2、CDK5 和 CDK9 (IC50=3/1/1/4 nM),具有选择性。Dinaciclib 具有潜在的抗肿瘤活性,可以抑制胸甘 (dThd) DNA 的整合。

规格价格库存数量
2 mg¥ 498现货
5 mg¥ 797现货
10 mg¥ 1,240现货
50 mg¥ 3,781现货
1 mL x 10 mM (in DMSO)¥ 877现货
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纯度:99.75%
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产品介绍

生物活性
产品描述
Dinaciclib (SCH 727965) is a CDK inhibitor that selectively inhibits CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). Dinaciclib has potential antitumor activity and inhibits the incorporation of thoracic glycan (dThd) DNA.
靶点活性
CDK1:3 nM (cell free), CDK5:1 nM (cell free), CDK9:4 nM (cell free), CDK2:1 nM (cell free)
体外活性
方法:人胰腺癌细胞系 MIAPaCa-2 和 Pa20C 用 Dinaciclib (0.5-128 nM) 处理 72 h,使用 MTT Assay 检测细胞活力。
结果:Dinaciclib 以剂量依赖的方式抑制 MIAPaCa-2 和 Pa20C 细胞的生长,GI50 分别约为 10 和 20 nM。[1]
方法:人骨肉瘤细胞系 SaOs-2 和 U2OS 用 Dinaciclib (5-62 nmol/L) 处理 4-24 h,使用 Western Blot 检测靶点蛋白表达水平。
结果:Dinaciclib 消除骨肉瘤细胞中 CDK 底物的磷酸化。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Dinaciclib (40 mg/kg,20% (w/v) HPBCD) 腹腔注射给携带人胰腺癌肿瘤 JH033 或 Panc286 的 CD1 nu/nu athymic 小鼠,每周两次,持续四周。
结果:Dinaciclib 抑制一组低渗透癌症异种移植物的体内生长。[1]
方法:为检测体内抗肿瘤活性,将 Dinaciclib (8-48 mg/kg) 腹腔注射给携带卵巢癌肿瘤 A2780 的 BALB/c 小鼠,每天一次,持续十天。
结果:Dinaciclib 在体内具有剂量依赖性的抗肿瘤活性,并且在低于 MTD 的剂量水平下几乎完全抑制肿瘤生长。[3]
激酶实验
Recombinant cyclin/CDK holoenzymes were purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes were typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mmol/L Tris-HCl (pH 8.0), 10 mmol/L MgCl2, 1 mmol/L DTT, and 0.1 mmol/L sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2-μmol/L substrate solution (a biotinylated peptide derived from histone H1) were mixed and combined with 10 μL of diluted SCH 727965. The reaction was started by the addition of 50 μL of 2 μmol/L ATP and 0.1 μCi of 33P-ATP. Kinase reactions were incubated for 1 hour at room temperature and were stopped by the addition of 0.1% Triton X-100, 1 mmol/L ATP, 5 mmol/L EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads were captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads were washed twice with 2 mol/L NaCl and twice with 2 mol/L NaCl containing 1% phosphoric acid. The signal was then assayed using a TopCount 96-well liquid scintillation counter. Dose-response curves were generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC50 values were derived by nonlinear regression analysis [1].
细胞实验
A2780 cells were plated into six-well tissue culture dishes and allowed to adhere. Cells were then exposed to differing concentrations of SCH 727965 or a DMSO control vehicle for 24 hours, followed by a brief (30 min) pulsed exposure to bromodeoxyuridine (BrdUrd). Cells were then harvested, immunostained using FITC-conjugated antibodies specific for BrdUrd, counter-stained with propidium iodide/RNase A solution, and analyzed using flow cytometry. Fluorescence-activated cell sorting analyses were done on a FACSCalibur instrument. FITC-positive BrdUrd staining and propidium iodide signal allowed assessment of ongoing DNA replication and the cell cycle stage. Percentages of the cell population in each cell cycle stage were plotted for each test article concentration [1].
动物实验
For tumor implantation, specific cell lines were grown in vitro, washed once with PBS, and resuspended in 50% Matrigel in PBS to a final concentration of 4 × 10^7 to 5 × 10^7 cells per milliliter. Nude mice were injected with 0.1 mL of this suspension s.c. in the flank region. Tumor length (L), width (W), and height (H) were measured by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L × W × H)/2. When the tumor volume reached ~100 mm^3, the animals were randomized to treatment groups (10 mice/group) and treated i.p. with either SCH 727965 or individual chemotherapeutic agents according to the dosing schedule indicated in table and figure legends. Tumor volumes and body weights were measured during and after the treatment periods. Data were expressed as means ± SEM. Animals were euthanized according to the Institutional Animal Care and Use Committee guidelines [1].
别名SCH 727965, PS-095760
化学信息
分子量396.49
分子式C21H28N6O2
CAS No.779353-01-4
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: 50 mg/mL (126.11 mM)
Ethanol: 8 mg/mL (20.17 mM), Heating is recommended.
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.5221 mL12.6107 mL25.2213 mL126.1066 mL
5 mM0.5044 mL2.5221 mL5.0443 mL25.2213 mL
10 mM0.2522 mL1.2611 mL2.5221 mL12.6107 mL
20 mM0.1261 mL0.6305 mL1.2611 mL6.3053 mL
DMSO
1mg5mg10mg50mg
50 mM0.0504 mL0.2522 mL0.5044 mL2.5221 mL
100 mM0.0252 mL0.1261 mL0.2522 mL1.2611 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
g
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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关键词

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