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Ro-3306

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产品编号 T2356Cas号 872573-93-8

Ro 3306 是一种 CDK1 抑制剂,可以抑制 CDK1、CDK1/cyclin B1 和 CDK2/cyclin E (Ki=20/35/340 nM),具有选择性和 ATP 竞争性。Ro-3306 具有抗肿瘤活性,可以抑制细胞周期阻滞,诱导细胞凋亡。

Ro-3306
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Ro-3306

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纯度: 99.74%
产品编号 T2356Cas号 872573-93-8

Ro 3306 是一种 CDK1 抑制剂,可以抑制 CDK1、CDK1/cyclin B1 和 CDK2/cyclin E (Ki=20/35/340 nM),具有选择性和 ATP 竞争性。Ro-3306 具有抗肿瘤活性,可以抑制细胞周期阻滞,诱导细胞凋亡。

规格价格库存数量
1 mg¥ 255现货
5 mg¥ 593现货
10 mg¥ 855现货
25 mg¥ 1,480现货
50 mg¥ 2,320现货
100 mg¥ 3,730现货
200 mg¥ 5,280现货
500 mg¥ 7,880现货
1 mL x 10 mM (in DMSO)¥ 683现货
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产品介绍

生物活性
产品描述
Ro 3306 is a CDK1 inhibitor that inhibits CDK1, CDK1/cyclin B1, and CDK2/cyclin E (Ki=20/35/340 nM) selectively and ATP-competitively. Ro-3306 exhibits antitumor activity, inhibits cell cycle arrest, and induces apoptosis.
靶点活性
CDK1:20 nM(Ki), PKCδ:318 nM(Ki), ERK:1980 nM(Ki), SGK:497 nM(Ki)
体外活性
方法:卵巢癌细胞 OVCA-429 和 OVCAR-3 用 Ro 3306 (1-2.5 nM) 处理 9 天,使用 crystal violet assay 检测细胞活力。
结果:OVCA-429 和 OVCAR-3 细胞在高剂量浓度的 Ro 3306 下长达 9 天的生长速率较低。使用 2.5 µM Ro 3306 处理,OVCA-429 和 OVCAR-3 细胞的生长率在第 9 天分别降低了 75.3% 和 87.7%。[1]
方法:人肿瘤细胞系 HCT116、SW480 和 HeLa 用 Ro 3306 (9 µM) 处理 20 h,使用 Flow cytometry 检测细胞周期。
结果:用 Ro 3306 对增殖的人类肿瘤细胞处理 20 h 导致 G2/M 期细胞周期的完全阻断。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Ro 3306 (4 mg/kg) 和 Cisplatin (4 mg/kg) 腹腔注射给携带卵巢癌肿瘤 OVCAR-3 的 BALB/c nude 小鼠,每四天一次,持续四周。
结果:与 Ro 3306 或 Cisplatin 治疗相比,联合治疗有效抑制了肿瘤生长。[1]
激酶实验
CDK assay: The activity of CDK1 cyclin B1, CDK1 cyclin A, CDK2 cyclin E, and CDK4 cyclin D is measured by a homogeneous time-resolved fluorescence assay in a 96-well format. The assay buffer contained 25 mM Hepes, 6.25 mM MgCl2, 0.003% Tween 20, 0.3 mg/mL BSA, 1.5 mM DTT, and ATP as follows: 162 μM (CDK1), 90 mM (CDK2), or 135 μM (CDK4). CDK1 and CDK2 buffer contained 10 mM MgCl2. Test compounds are diluted in assay buffer to 3-fold their final concentration in 20 μL, and the reaction is started by the addition of a 40 μL assay buffer containing the pRB substrate (0.185 μM). The plates are incubated at 37°C for 30 min with constant agitation, and the reaction is terminated by the addition of 15 μL of 1.6 μM anti-phospho pRB antibody (Ser-780) in 25 mM Hepes, 24 mM EDTA, and 0.2 mg/mL BSA. After an additional 30 min of incubation with shaking, 15μL of 3 nM Lance-Eu-W1024-labeledanti-rabbitIgG and 60 nM Alophycocyanin-conjugated anti-His-6 antibody in 25 mM Hepes, and 0.5 mg/mL BSA is added and incubated for 1 h. The plates are read in the Victor-V multi- label reader at excitation 340 nm and emission 615 nm and 665 nm. The IC50 values are calculated from the readings at 665 nm and normalized for Europium readings at 615 nm. Ki values are calculated according to the equation: Ki= IC50/(1 + S/Km ), where S is the ATP concentration in the assay and Km is the Michaelis-Menten constant for ATP. The inhibitory activity against the panel of kinases is determined by the IMAP assay technology.
细胞实验
Log phases cells (25,000) are seeed in 96-well plates and incubated in a 37℃ incubator with CO2, After 24 h, different concentrations of RO-3306 are administered to determine the drug concentrations required to achieve a 50% growth inhibition (IC50). MTT (20 μL, 5 mg/mL stock solution in saline) is added to each well and the cells are incubated for 4 h. Supernatants are removed and formazan crystals from viable cells are solubilized with 200 μL anhydrous DMSO. The absorbance is detected with a 550 model microplate reader at the 565 nm wavelength.(Only for Reference)
化学信息
分子量351.45
分子式C18H13N3OS2
CAS No.872573-93-8
SmilesO=C1N=C(NCc2cccs2)SC1=Cc1ccc2ncccc2c1
密度1.41 g/cm3
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: 12.5 mg/mL (35.57 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1.25 mg/mL (3.56 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
溶液配制表
1mg5mg10mg50mg
1 mM2.8454 mL14.2268 mL28.4535 mL142.2677 mL
1mg5mg10mg50mg
5 mM0.5691 mL2.8454 mL5.6907 mL28.4535 mL
10 mM0.2845 mL1.4227 mL2.8454 mL14.2268 mL
20 mM0.1423 mL0.7113 mL1.4227 mL7.1134 mL

计算器

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  • 稀释 计算器
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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
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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
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%Tween 80
%ddH2O

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