Carboxyamidotriazole Orotate

SKU: orb1218562

Description

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.

Key Properties

• CAS Number: 187739-60-2
• MW: 580.76
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₆Cl₃N₇O₆
• SMILES: 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
• Target: Calcium Channel
• Solubility: DMSO:5 mg/mL (8.61 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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.
• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

L-651582 Orotate | CAI Orotate

Quick Database Links

Gene Symbol

Calcium Channel