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Carboxyamidotriazole (L-651582) is an orally active cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole inhibits NF-κB, MAPK activation and NO production. Carboxyamidotriazole has anti-angiogenic and anti-inflammatory activities. Carboxyamidotriazole has anticancer activity against liver cancer, lung cancer and leukemia.
For research use only. We do not sell to patients.
Carboxyamidotriazole (L-651582) is an orally active cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole inhibits NF-κB, MAPK activation and NO production. Carboxyamidotriazole has anti-angiogenic and anti-inflammatory activities. Carboxyamidotriazole has anticancer activity against liver cancer, lung cancer and leukemia[1][2][3][4][5][6][7][8][9][10][11][12][13].
Carboxyamidotriazole (10 μM; 15 min) suppresses mitochondrial calcium import in Digitonin (HY-N4000)-permeabilized HEK -293 cells[2].
Carboxyamidotriazole (24 h) inhibits the proliferation of HepG2 and Huh-7 cells, with IC50s of 0.7 μM and 4.5 μM, respectively, as measured by [3H]thymidine incorporation[3].
Carboxyamidotriazole (10-20 μM; 48 h) dose-dependently inhibits the viability of LLC cells and promotes glucose uptake and lactate production in them[4].
Carboxyamidotriazole (1-40 μM; 0-5 days) inhibited cell growth in a dose- and time-dependent manner in a proliferation assay of human chronic myeloid leukemia (CML) cell lines (LAMA84R, K562R, KCL22R)[7].
Carboxyamidotriazole (10-40 μM; pretreatment for 2 h, then co-stimulation with LPS for 6 h) reduced NO production and iNOS expression and downregulated proinflammatory cytokine levels in mouse RAW264.7 macrophages[8].
Carboxyamidotriazole (5-40 μM, 48 h) inhibited the proliferation of fibroblast-like synoviocytes in a rat adjuvant arthritis model[9].
Carboxyamidotriazole (1.25-40 μM; 48-72 h) significantly inhibits the proliferation of Lewis lung carcinoma (LLC) cells[10].
Carboxyamidotriazole (10 μM; 24 h) enhances the cytotoxicity of cytotoxic T lymphocytes (CTLs) and promotes the release of IFN-γ in the co-culture experiment of mouse B16 melanoma cells and CTLs[12].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pretreatment for 2 h and then co-stimulation with LPS for different times (6 h for iNOS detection, 1 h for NF-κB and MAPK analysis)
Result:
Reduced iNOS expression.
Inhibited NF-κB activation and MAPK activation.
In Vivo
Carboxyamidotriazole (30 mg/kg; i.g.; daily; 19 days) combined with 2-deoxyglucose retards the growth of LLC tumors in C57BL/6 mice[4].
Carboxyamidotriazole (10-40 mg/kg; i.g.; once daily; from day 12 to day 26 after arthritis induction) reduces the severity of arthritis, inhibits hind paw swelling, decreases the infiltration of joint pathological inflammatory cells in the adjuvant arthritis model of Lewis rats induced by complete Freund's adjuvant[9].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; from day 7 to day 29 after inoculation of tumor cells) inhibits tumor growth, enhances the weights of gastrocnemius muscle and epididymal adipose tissue in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells[10].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; for 29 days) combined with low-dose Sorafenib (HY-10201) synergistically inhibits tumor growth in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells[11].
Carboxyamidotriazole (20 mg/kg; i.g.; once daily) combined with 1-MT or DMF, increases the number of CD8+ T cells in tumor-infiltrating lymphocytes (TILs), enhances the anti-tumor immune response of T cells, inhibits tumor growth, and prolongs the survival in the C57BL/6, BALB/c or RAG1 KO mouse models inoculated with B16, C26, 4T1 or B16-OVA tumor cells[12].
Carboxyamidotriazole (40 mg/kg, p.o., once daily, 14 days) reduces Bleomycin (HY-108345)-induced lung injury in mice[13].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Carboxyamidotriazole (30 mg/kg, dissolved in PEG 400), 2-DG (450 mg/kg)
Administration:
Carboxyamidotriazole was administered intragastrically daily, and 2-DG was administered intraperitoneally daily for 19 days
Result:
Caused no obvious changes in the animal body weight and behaviors.
Resulted in slower tumor growth than in the groups treated with Carboxyamidotriazole or 2-DG alone.
Animal Model:
C57BL/6J male mice (weight: 18-22 g, 6-8 weeks old) inoculated with Lewis lung carcinoma cells[11]
Dosage:
30 mg/kg
Administration:
Intragastric administration, once daily, 29 days
Result:
Synergistically inhibited tumor growth in combination with low-dose Sorafenib.
Showed comparable efficacy to high-dose Sorafenib monotherapy.
Alleviated weight loss during cancer progression and inhibited NANOG expression in tumor tissues.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (235.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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