Carboxyamidotriazole Orotate

Research use only, not for human use.

Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways.

Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-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. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.(In Vitro):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.(In Vivo):Carboxyamidotriazole Orotate (342, 513 mg/kg; i.p.; Q1D×5 for two rounds) displays antitumor activity on CML xenografts.

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.

L-651582 Orotate | CAI Orotate

GPCR/G Protein

Calcium Channel

Calcium Channel

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187739-60-2

580.76

C22H16Cl3N7O6

>98% (HPLC)

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

O=C(C(NC1=O)=CC(N1)=O)O.O=C(C2=C(N)N(CC3=CC(Cl)=C(C(C4=CC=C(Cl)C=C4)=O)C(Cl)=C3)N=N2)N

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(-20℃)

With Ice Pack

≥ 2 years