Carboxyamidotriazole Orotate

Modify Date: 2024-01-12 19:41:22

Carboxyamidotriazole Orotate Structure
Carboxyamidotriazole Orotate structure
Common Name Carboxyamidotriazole Orotate
CAS Number 187739-60-2 Molecular Weight 580.765
Density N/A Boiling Point N/A
Molecular Formula C22H16Cl3N7O6 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Carboxyamidotriazole Orotate


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].

 Names

Name 776C212QQH
Synonym More Synonyms

 Carboxyamidotriazole Orotate Biological Activity

Description 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].
Related Catalog
In Vitro Carboxyamidotriazole Orotate (0.1-10 µM; 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 µM Carboxyamidotriazole Orotate treatment[1]. Cell Viability Assay[1] 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[1] 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.
In Vivo Carboxyamidotriazole Orotate (342, 513 mg/kg; i.p.; Q1D×5 for two rounds) displays antitumor activity on CML xenografts[1]. Animal Model: Male NOD/SCID mice four-to-five week old[1] Dosage: 342, 513 mg/kg Administration: i.p.; Q1D×5 for two rounds Result: Increase survival.
References

[1]. Corrado C, et al. Carboxyamidotriazole-orotate inhibits the growth of imatinib-resistant chronic myeloid leukaemia cells and modulates exosomes-stimulated angiogenesis. PLoS One. 2012;7(8):e42310.

[2]. Hussain MM, et al. Phase II trial of carboxyamidotriazole in patients with relapsed epithelial ovarian cancer. J Clin Oncol. 2003 Dec 1;21(23):4356-63.

 Chemical & Physical Properties

Molecular Formula C22H16Cl3N7O6
Molecular Weight 580.765
Exact Mass 579.022766

 Safety Information

Hazard Codes Xi

 Synonyms

2,6-Dioxo-1,2,3,6-tetrahydro-4-pyrimidinecarboxylic acid - 5-amino-1-[3,5-dichloro-4-(4-chlorobenzoyl)benzyl]-1H-1,2,3-triazole-4-carboxamide (1:1)
4-Pyrimidinecarboxylic acid, 1,2,3,6-tetrahydro-2,6-dioxo-, compd. with 5-amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]-1H-1,2,3-triazole-4-carboxamide (1:1)
776C212QQH
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