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Ro-3306

Ro-3306

产品编号 T2356   CAS 872573-93-8

Ro 3306 是一种选择性 ATP 竞争性CDK1抑制剂,对 CDK1、CDK1/cyclin B1 和 CDK2/cyclin E 的Ki 值为分别为 20 nM、35 nM 和 340 nM。

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Ro-3306 Chemical Structure
Ro-3306, CAS 872573-93-8
规格 价格/CNY 货期 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 * 10 mM (in DMSO) ¥ 683 现货
产品目录号及名称: Ro-3306 (T2356)
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选择批次  
纯度: 99.74%
纯度: 98.59%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.
靶点活性 CDK1:20 nM(Ki), PKCδ:318 nM(Ki), ERK:1980 nM(Ki), SGK:497 nM(Ki)
体内活性 在HCT116,SW480和HeLa细胞中,RO-3306处理20小时后,细胞周期完全阻滞在G2/M期。 RO-3306(10 μM)有效阻止卵母细胞成熟。RO-3306抑制CDK1/cyclin B1(Ki:35 nM),CDK1/cyclin A(Ki:110 nM),CDK2/cyclin E(Ki:340 nM),和CDK4/cyclin D(Ki>2000 nM)活性。RO-3306可有效阻断HCT116和SW480的增殖。与非致瘤性细胞(MCF 10A和MCF 12A)相比,RO-3306似乎对癌细胞(HCT116和SW480)的促凋亡作用更强。
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)
分子量 351.45
分子式 C18H13N3OS2
CAS No. 872573-93-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 12.5 mg/mL (35.57 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8454 mL 14.2268 mL 28.4535 mL 71.1339 mL
5 mM 0.5691 mL 2.8454 mL 5.6907 mL 14.2268 mL
10 mM 0.2845 mL 1.4227 mL 2.8454 mL 7.1134 mL
20 mM 0.1423 mL 0.7113 mL 1.4227 mL 3.5567 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
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参考文献

1. Vassilev LT, et al. Proc Natl Acad Sci U S A. 2006, 103(28), 10660-10665. 2. Jang WI, et al. Anim Reprod Sci. 2014, 144(3-4), 102-108. 3. Xia Q, et al. Int J Oncol. 2014, 44(3), 735-744. 4. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

文献引用

1. Zhang Y, Hong X, Hua S, et al. Reconstitution and mechanistic dissection of the human microtubule branching machinery. Journal of Cell Biology. 2022, 221(7): e202109053 2. Chen C, Zhang X, Wang Y, et al. Translational and Post-translational Control of Human Naïve versus Primed Pluripotency. iScience. 2021: 103645. 3. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity. Biochemical and Biophysical Research Communications. 2019 Jun 11;513(4):967-973 4. Guo S, Lei X, Chang Y, et al.SARS-CoV-2 hijacks cellular kinase CDK2 to promote viral RNA synthesis.Signal Transduction and Targeted Therapy.2022, 7(1): 1-12. 5. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642.
Bisacurone Cimiside E Daphnetin 6-Deoxyisojacareubin Afuresertib Leucosceptoside A SU9516 A-674563 2HCl(552325-73-2(fb-2hcl))

相关化合物库

该产品包含在如下化合物库中:
TGF-β/Smad靶点化合物库 酪氨酸激酶分子库 HIF-1化合物库 抗衰老化合物库 抗卵巢癌化合物库 成骨分子库 MAPK 抑制剂库 ReFRAME 相关化合物库 自噬库 抗前列腺癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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: 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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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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技术支持

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。

Keywords

Ro-3306 872573-93-8 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling MAPK Metabolism Tyrosine Kinase/Adaptors ERK SGK PKA CDK PKC Cyclin dependent kinase Ro3306 Inhibitor Ro 3306 inhibit inhibitor

 

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