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COH29

COH29

产品编号 T3157   CAS 1190932-38-7
别名: RNR Inhibitor COH29

COH29 (RNR Inhibitor COH29) 是一种口服可用的芳香族取代噻唑,是人类核糖核苷酸还原酶 (RNR) 的抑制剂,具有潜在的抗肿瘤活性。它抑制核糖核苷酸还原酶的IC50为 16 μM。

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COH29 Chemical Structure
COH29, CAS 1190932-38-7
规格 价格/CNY 货期 数量
1 mg ¥ 768 现货
2 mg ¥ 1,130 现货
5 mg ¥ 1,890 现货
10 mg ¥ 2,820 现货
25 mg ¥ 4,590 现货
50 mg ¥ 6,450 现货
100 mg ¥ 8,680 现货
1 mL * 10 mM (in DMSO) ¥ 2,080 现货
产品目录号及名称: COH29 (T3157)
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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 COH29 (RNR Inhibitor COH29) is an orally available, aromatically substituted thiazole and inhibitor of the human ribonucleotide reductase (RNR), with potential antineoplastic activity. Upon oral administration, the RNR inhibitor COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail. Inhibition of RNR activity decreases the pool of deoxyribonucleotide triphosphates available for DNA synthesis. The resulting decrease in DNA synthesis causes cell cycle arrest and growth inhibition. In addition, this agent may inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, which prevents the repair of damaged DNA and causes both the accumulation of single and double strand DNA breaks and the induction of apoptosis.
靶点活性 RNR:16 μM.
体外活性 COH29 overcome gemcitabine and hydroxyurea resistance in Y cells. It potently inhibits proliferation of most cell lines in the NCI 60 human Y panel, most especially leukemia and ovarian Y, but exerts little effect on normal fibroblasts or endothelial cells. NMR, site-directed mutagenesis, and surface plasmon resonance biosensor studies confirm COH29 binding to the proposed ligand-binding pocket and offer evidence for assembly blockade of the RRM1-RRM2 quaternary structure[1].
体内活性 COH29 (50/100 mg/kg, b.i.d., p.o.)results in a dose-dependent inhibition of MOLT-4 tumor xenograft growth, which is pronounced by Day 12 of treatment. In mice bearing TOV11D xenografts, 7 days of treatment with COH29 (200/300/400 mg/kg/day) results in a dose-dependent inhibition of tumor xenograft growth. Compared with the control group, tumor growth is significantly inhibited [1].
激酶实验 For kinase assays following immunoprecipitation of FLAG-CDK7 protein from HCT116 or FLAG-CDK12 from 293A cellular lysates, cells are first treated with THZ1, THZ1-R, or DMSO for 4 hrs at 37°C. Cells are then harvested by lysis in 50 mM Tris HCl pH 8.0, 150 mM NaCl, 1% NP-40, 5 mM EDTA, and protease/phosphatase cocktails. Exogenous CDK7 or CDK12 proteins are immunoprecipitated from cellular lysates using FLAG antibody- conjugated agarose beads. Precipitated proteins are washed with lysis buffer 6 times, followed by 2 washes with kinase buffer (40 mM Hepes pH 7.5, 150 mM NaCl, 10 mM MgCl2, 5% glycerol) and subjected to in vitro kinase assays at 30°C for 45 minutes using 1 μg of the large subunit of RNAPII (RPB1) as substrate and 25 μM ATP and 10 μCi of 32P ATP. Kinase assays using recombinant CDK7/TFIIH/MAT1 are conducted in the manner as described above using 25 ng of CAK complex per reaction. For kinase assays designed to test time-dependent inactivation of CDK7 kinase activity, CAK complex is pre-incubated with indicated concentrations of THZ1, THZ1-R, or DMSO in kinase buffer without ATP for 4 hrs at 30°C prior to being subjected to kinase assay conditions[1].
细胞实验 Cells is seeded into 96-well plates in 100 μL of complete medium at 2000 to 5000 cells per well, depending on the cell line's growth rate. After overnight incubation, test compound is added to each well at various concentrations in 50 μL of culture medium. After a further incubation for 96 hours at 37°C, fluorescein diacetate (final concentration: 10 mg/mL) and eosin Y [final concentration: 0.1% (w/v)] is added to each well, and the cells is incubated for an additional 20 minutes at 37°C. Cytotoxicity is assessed by Digital Imaging Microscopy System detection Viability is assessed using MTS [(3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium)] as previously described[1].
别名 RNR Inhibitor COH29
分子量 420.44
分子式 C22H16N2O5S
CAS No. 1190932-38-7

存储

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

溶解度

DMSO: 50 mg/mL (118.92 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 2.3785 mL 11.8923 mL 23.7846 mL 59.4615 mL
5 mM 0.4757 mL 2.3785 mL 4.7569 mL 11.8923 mL
10 mM 0.2378 mL 1.1892 mL 2.3785 mL 5.9462 mL
20 mM 0.1189 mL 0.5946 mL 1.1892 mL 2.9731 mL
50 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 mL
100 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5946 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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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Zhou B, et al. A small-molecule blocking ribonucleotide reductase holoenzyme formation inhibits cancer cell growth and overcomes drug resistance.Cancer Res. 2013 Nov 1;73(21):6484-93. 2. Chen MC, et al. The Novel Ribonucleotide Reductase Inhibitor COH29 Inhibits DNA Repair In Vitro. Mol Pharmacol. 2015 Jun;87(6):996-1005.

文献引用

1. Wang R, Xu Z, Tian J, et al. Pterostilbene inhibits hepatocellular carcinoma proliferation and HBV replication by targeting ribonucleotide reductase M2 protein. American Journal of Cancer Research. 2021, 11(6): 2975.
NKP-1339 Azelaic acid IDD388 Halofuginone hydrobromide 6-AZATHYMINE AI-10-49 Carboplatin O6-Benzylguanine

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 抗癌临床化合物库 抗衰老化合物库 抗COVID-19化合物库 毒性化合物库 药物功能重定位化合物库 口服活性化合物库 ReFRAME 相关化合物库 经典已知活性库

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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% 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

COH29 1190932-38-7 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis ribonucleotide RNR inhibit reductase RNR Inhibitor COH29 RNR Inhibitor COH-29 subunit RNR Inhibitor COH 29 COH-29 Inhibitor COH 29 anticancer inhibitor

 

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