187739-60-2
中文名稱
CARBOXYAMIDOTRIAZOLE OROTATE
英文名稱
CARBOXYAMIDOTRIAZOLE OROTATE
CAS
187739-60-2
分子式
C22H16Cl3N7O6
分子量
580.765
MOL 文件
187739-60-2.mol
更新日期
2023/03/20 15:41:25
187739-60-2 結(jié)構(gòu)式
基本信息
中文別名
化合物CARBOXYAMIDOTRIAZOLE OROTATE 英文別名
CAI OrotateL-651582 Orotate
OCSMDRBVJRAMCI-UHFFFAOYSA-N
CARBOXYAMIDOTRIAZOLE OROTATE
常見問題列表
生物活性
Carboxyamidotriazole Orotate (L-651582 Orotate)，是一種口服生物有效的信號轉(zhuǎn)導抑制劑Carboxyamidotriazole (CAI) 的 orotate 鹽形式。Carboxyamidotriazole Orotate 是一種非電壓性鈣通道 (nonvoltage-operated calcium channels) 和鈣通道介導的信號通路 (calcium channel-mediated signaling pathways) 的細胞抑制劑，具有抗癌，抗炎活性和抗血管生成作用。體外研究
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. |
體內(nèi)研究
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. |