Carboxyamidotriazole (Orotate)

187739-60-2

580.76

DMSO : 5 mg/mL (8.61 mM; Need ultrasonic)

Membrane Transporter/Ion Channel; Neuronal Signaling

Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects^[1][2]. In Vitro: Carboxyamidotriazole Orotate (0.1-10 uM; 24-96 hours) inhibits cell proliferation of LAMA84R and K562R cell lines^[1].
Carboxyamidotriazole Orotate inhibits the phosphorylation of a selected target of Bcr-Abl kinase. Tyrosine phosphorylation of CrkL is reduced by 5 uM Carboxyamidotriazole Orotate treatment^[1]. In Vivo: Carboxyamidotriazole Orotate (342, 513 mg/kg; i.p.; Q1Dx5 for two rounds) displays antitumor activity on CML xenografts^[1].