Size | Price | Stock | Qty |
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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 |
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Carboxyamidotriazole orotate is the orotate salt form of carboxyamidotriazole (CAI; RFE-007; L-651582; NSC-609974), which is a novel and potent inhibitor of both cAMP-phosphodiesterases and GMP-phosphodiesterases with anti-tumor, antiangiogenic and anti-inflammatory activity. Also an inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways.
ln Vitro |
In LAMA84R and K562R cell lines, carboxyamidotriaz orotate (0.1–10 µM; 24-96 hours) suppresses cell proliferation [1]. Bcr-Abl kinase phosphorylation of specific sites is inhibited by carboxyamidotriaz otate. The application of 5 µM carboxamide triazole orotate inhibits CrkL's tyrosine phosphorylation [1].
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ln Vivo |
CML xenografts were subjected to carboxamide triazole orotate (342, 513 mg/kg; i.p.; two rounds Q1D×5), which exhibited anticancer efficacy [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: LAMA84R and K562R Cell lines Tested Concentrations: 0.1, 1, 5, 10 µM Incubation Duration: 24, 48, 72, 96 hrs (hours) Experimental Results: Shows 50% reduction in chronic myelogenous leukemia (CML) growth) Line with 5 µM CTO at the 96 hour time point. Western Blot Analysis[1] Cell Types: LAMA84R and K562R cell lines Tested Concentrations: 0.1, 1, 5 µM Incubation Duration: 72 and 96 hrs (hours) Experimental Results: Dose-dependent inhibition of total Bcr-Abl levels and phosphorylated Bcr-Abl levels. |
Animal Protocol |
Animal/Disease Models: Four to five week old male NOD/SCID (severe combined immunodeficient) mouse [1]
Doses: 342, 513 mg/kg Route of Administration: intraperitoneal (ip) injection; Q1D×5 two-round Experimental Results: increased survival rate. |
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. |
Molecular Formula |
C22H16CL3N7O6
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Molecular Weight |
580.764740943909
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CAS # |
187739-60-2
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Related CAS # |
Carboxyamidotriazole;99519-84-3
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SMILES |
ClC1C(C(C2C=CC(=CC=2)Cl)=O)=C(C=C(C=1)CN1C(=C(C(N)=O)N=N1)N)Cl.O=C1C(C(=O)O)=CNC(N1)=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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 : ~5 mg/mL (~8.61 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7219 mL | 8.6094 mL | 17.2188 mL | |
5 mM | 0.3444 mL | 1.7219 mL | 3.4438 mL | |
10 mM | 0.1722 mL | 0.8609 mL | 1.7219 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.