CARBOXYAMIDOTRIAZOLE OROTATE
| 中文名称 | CARBOXYAMIDOTRIAZOLE OROTATE |
|---|---|
| 中文同义词 | 化合物CARBOXYAMIDOTRIAZOLE OROTATE |
| 英文名称 | CARBOXYAMIDOTRIAZOLE OROTATE |
| 英文同义词 | CARBOXYAMIDOTRIAZOLE OROTATE;OCSMDRBVJRAMCI-UHFFFAOYSA-N;CAI Orotate;L-651582 Orotate;L651582,Inhibitor,toxicity,Calcium Channel,L 651582,Ca2+ channels,Ca channels,leukaemia,inhibit,ovarian,chronic,Carboxyamidotriazole,Carboxyamidotriazole Orotate,CAI,Bcr/Abl,L-651582,cancer,myelogenous |
| CAS号 | 187739-60-2 |
| 分子式 | C22H16Cl3N7O6 |
| 分子量 | 580.76 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 187739-60-2.mol |
| 结构式 |  |
CARBOXYAMIDOTRIAZOLE OROTATE 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：5 mg/mL（8.61 mM） |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
Carboxyamidotriazole Orotate (L-651582 Orotate)，是一种口服生物有效的信号转导抑制剂Carboxyamidotriazole (CAI) 的 orotate 盐形式。Carboxyamidotriazole Orotate 是一种非电压性钙通道 (nonvoltage-operated calcium channels) 和钙通道介导的信号通路 (calcium channel-mediated signaling pathways) 的细胞抑制剂，具有抗癌，抗炎活性和抗血管生成作用。
Carboxyamidotriazole Orotate (0.1-10 µM; 24-96 hours) inhibits cell proliferation of LAMA84R and K562R cell lines.
Carboxyamidotriazole Orotate inhibits the phosphorylation of a selected target of Bcr-Abl kinase. Tyrosine phosphorylation of CrkL is reduced by 5 µM Carboxyamidotriazole Orotate treatment.
Cell Viability Assay
| Cell Line: | LAMA84R and K562R cell lines |
| Concentration: | 0.1, 1, 5, 10 µM |
| Incubation Time: | 24, 48, 72, 96 hours |
| Result: | Showed a 50% growth reduction of the chronic myelogenous leukaemia (CML) lines with 5 µM CTO at 96 h time point. |
Western Blot Analysis
| Cell Line: | LAMA84R and K562R cell lines |
| Concentration: | 0.1, 1, 5 µM |
| Incubation Time: | 72 and 96 hours |
| Result: | A dose-dependent inhibition of both total and phosphorylated Bcr-Abl levels. |
Carboxyamidotriazole Orotate (342, 513 mg/kg; i.p.; Q1D×5 for two rounds) displays antitumor activity on CML xenografts.
| Animal Model: | Male NOD/SCID mice four-to-five week old |
| Dosage: | 342, 513 mg/kg |
| Administration: | i.p.; Q1D×5 for two rounds |
| Result: | Increase survival. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-16125 | CARBOXYAMIDOTRIAZOLE OROTATE Carboxyamidotriazole Orotate | 187739-60-2 | 5mg | 2000元 |
| 2024/04/30 | S2975 | CarboxyaMidotriazole orotate | 187739-60-2 | 5mg | 2211.3元 |