CarboxyamIDOtriazole Orotate 是一种可口服的信号转导抑制剂，是CarboxyamIDOtriazole (CAI) 的乳清酸盐形式。它是一种非电压性钙通道和钙通道介导的信号通路的细胞抑制剂，具有抗癌、抗炎活性和抗血管生成作用。

Carboxyamidotriazole Orotate is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor that in vitro has been shown to possess antileukaemic activities. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory, and antiangiogenic effects.

Carboxyamidotriazole Orotate inhibits the phosphorylation of a selected target of Bcr-Abl kinase. Carboxyamidotriazole Orotate (0.1-10 μM; 24-96 hours) inhibits cell proliferation of LAMA84R and K562R cell lines[1]. Tyrosine phosphorylation of CrkL is reduced by 5 μM Carboxyamidotriazole Orotate treatment[1].

On CML xenografts, Carboxyamidotriazole Orotate (342, 513 mg/kg; i.p.; Q1D×5 for two rounds) shows antitumor activity[1].

187739-60-2

C22H16Cl3N7O6

580.77

CAI Orotate;L-651582 Orotate

DMSO:5 mg/mL (8.61 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years