187739-60-2
187739-60-2 structure
- Name: Carboxyamidotriazole Orotate
- Chemical Name: 776C212QQH
- CAS Number: 187739-60-2
- Molecular Formula: C22H16Cl3N7O6
- Molecular Weight: 580.765
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
- Create Date: 2018-07-10 23:55:28
- Modify Date: 2024-01-12 19:41:22
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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].
| Name | 776C212QQH |
|---|---|
| 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 |
| 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 |
| Molecular Formula | C22H16Cl3N7O6 |
|---|---|
| Molecular Weight | 580.765 |
| Exact Mass | 579.022766 |
| Hazard Codes | Xi |
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