| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
Purity: =97.97%
| Targets |
Carboxyamidotriazole's primary target is non-voltage-operated calcium channels, including store-operated calcium channels (SOCs) and receptor-operated calcium channels (ROCs). By inhibiting these channels, it reduces calcium influx and downstream signaling pathways, including NF-κB activation. The compound inhibits oxidative phosphorylation in cancer cells, which is a key metabolic pathway for ATP production. It also inhibits the production of pro-inflammatory cytokines in tumor-associated macrophages. These multiple mechanisms contribute to its anti-tumor, anti-inflammatory, and anti-angiogenic effects.
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| ln Vitro |
In vitro, Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. It inhibits oxidative phosphorylation in cancer cells and exerts synergistic anti-cancer effects with glycolysis inhibition. The compound shows anti-tumor, anti-inflammatory, and anti-angiogenic effects in various cell-based assays. It synergizes with Bay 43-9006 (sorafenib) to combat non-small cell lung cancer through inhibition of NANOG and aggravation of apoptosis. Carboxyamidotriazole inhibits the production of pro-inflammatory cytokines in tumor-associated macrophages.
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| ln Vivo |
In vivo, Carboxyamidotriazole is an orally active compound that has been studied for its anti-tumor and anti-inflammatory effects. It ameliorates experimental colitis by inhibiting cytokine production, NF-κB activation, and colonic fibrosis. The compound has anticancer activity against liver cancer, lung cancer, and leukemia in preclinical models. Its ability to inhibit angiogenesis contributes to its anti-tumor effects by reducing tumor blood supply. Carboxyamidotriazole has been investigated in clinical trials for the treatment of various cancers.
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| Enzyme Assay |
The in vitro activity of Carboxyamidotriazole is assessed using various cell-based assays. For calcium channel inhibition studies, cells are loaded with a calcium-sensitive fluorescent dye (e.g., Fura-2 or Fluo-4) and stimulated with agents that activate store-operated or receptor-operated calcium channels (e.g., thapsigargin, ATP). The inhibition of calcium influx by Carboxyamidotriazole is measured using a fluorescence plate reader. For anti-tumor studies, various cancer cell lines are treated with Carboxyamidotriazole (typically 1-100 µM) for 24-72 hours, and cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by measuring caspase-3/7 activity or by flow cytometry. For anti-angiogenic studies, endothelial cell tube formation assays are performed.
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| Cell Assay |
For cellular assays, cancer cell lines (e.g., HepG2, A549, MCF-7) and endothelial cells (e.g., HUVECs) are used. Cells are cultured in appropriate media and treated with various concentrations of Carboxyamidotriazole (typically 1-100 µM) for defined periods. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining or by measuring caspase-3/7 activity. Cell cycle progression is analyzed by flow cytometry using propidium iodide staining. The production of pro-inflammatory cytokines (e.g., TNF-α, IL-6) is measured by ELISA. NF-κB activation is assessed by Western blotting or by using a NF-κB reporter assay.
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| Animal Protocol |
In vivo, Carboxyamidotriazole is typically administered orally to animal models. For anti-tumor studies, mice bearing tumor xenografts are treated with Carboxyamidotriazole at various doses (typically 10-100 mg/kg) daily for 2-4 weeks. Tumor growth is monitored by measuring tumor volume. For anti-inflammatory studies, animal models of colitis (e.g., DSS-induced colitis) are treated with Carboxyamidotriazole, and disease severity is assessed by clinical scoring, histopathology, and measurement of inflammatory markers.
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| ADME/Pharmacokinetics |
Carboxyamidotriazole is orally active. It has a molecular weight of 424.67 g/mol and a molecular formula of C17H12Cl3N5O2. The compound is soluble in DMSO at 10 mg/mL. It should be stored at -20°C under appropriate conditions to maintain stability. Specific pharmacokinetic data (absorption, distribution, metabolism, excretion) is not detailed in the provided search results. Its bioavailability and half-life would require further investigation.
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| Toxicity/Toxicokinetics |
Carboxyamidotriazole is generally well-tolerated in animal studies at therapeutic doses. Common side effects may include gastrointestinal disturbances, fatigue, and dizziness. As a calcium channel blocker, it may affect cardiovascular function, including blood pressure and heart rate. The compound should be used with caution in patients with cardiovascular disease. Its anti-angiogenic effects may impair wound healing. Comprehensive toxicological studies are required to establish its full safety profile.
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| References | |
| Additional Infomation |
Carboxyamidotriazole has been used in clinical trials for the treatment of various cancers, including lymphoma, lung cancer, breast cancer, kidney cancer, and ovarian cancer. Carboxyamidotriazole is an orally active drug with potential antitumor activity. It binds to and inhibits the activity of non-voltage-gated calcium channels, thereby blocking calcium ion inflow into cells and release from intracellular calcium stores, leading to the disruption of calcium channel-mediated signal transduction and inhibiting vascular endothelial growth factor (VEGF) signaling, endothelial cell proliferation, and angiogenesis. This drug may also inhibit tumor cell growth, invasion, and metastasis. (NCI04)
Carboxyamidotriazole is an investigational compound that has been studied for its potential therapeutic applications in cancer and inflammatory diseases. It has been investigated in clinical trials for the treatment of various cancers, including ovarian cancer, breast cancer, and non-small cell lung cancer. The compound's mechanism of action involves inhibition of calcium channels, oxidative phosphorylation, and NF-κB activation. Its anti-angiogenic effects make it a candidate for combination therapy with other anticancer agents. Carboxyamidotriazole is not approved for clinical use in most countries and is intended for research purposes. It is available from chemical suppliers for research applications. |
| Molecular Formula |
C17H12CL3N5O2
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| Molecular Weight |
424.67
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| Exact Mass |
423.006
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| CAS # |
99519-84-3
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| Related CAS # |
Carboxyamidotriazole Orotate;187739-60-2
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| PubChem CID |
108144
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| Appearance |
White to off-white solid powder
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| Density |
1.65g/cm3
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| Boiling Point |
685.5ºC at 760 mmHg
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| Flash Point |
368.3ºC
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| Index of Refraction |
1.73
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| LogP |
4.48
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WNRZHQBJSXRYJK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12Cl3N5O2/c18-10-3-1-9(2-4-10)15(26)13-11(19)5-8(6-12(13)20)7-25-16(21)14(17(22)27)23-24-25/h1-6H,7,21H2,(H2,22,27)
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| Chemical Name |
5-amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]triazole-4-carboxamide
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| Synonyms |
RFE007L651582NSC609974RFE-007L-651582NSC-609974NSC 609974 RFE 007 CAI
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~235.48 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3548 mL | 11.7738 mL | 23.5477 mL | |
| 5 mM | 0.4710 mL | 2.3548 mL | 4.7095 mL | |
| 10 mM | 0.2355 mL | 1.1774 mL | 2.3548 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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