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> Carboxyamidotriazole [99519-84-3]

Carboxyamidotriazole [99519-84-3]

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Referencia HY-16126-25mg

embalaje : 25mg

Marca : MedChemExpress

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Descripciòn

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].

IC50 & Target

Calcium channel[1]
Cellular Effect
Cell Line Type Value Description References
Caco-2 CC50
0.11 μM
Compound: CARBOXYAMIDOTRIAZOLE
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
Caco-2 IC50
0.09 μM
Compound: CARBOXYAMIDOTRIAZOLE
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
In Vitro

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.

Carboxyamidotriazole Related Antibodies

Western Blot Analysis[8]

Cell Line: RAW264.7 macrophages
Concentration: 10, 20 40 μM
Incubation Time: 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.

Animal Model: C57BL/6 mice (weight: 18-22 g) + LLC xenograft model[4]
Dosage: 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.
Peso molecular

424.67

Fòrmula

C17H12Cl3N5O2
No. CAS
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=C(N)N(CC2=CC(Cl)=C(C(C3=CC=C(Cl)C=C3)=O)C(Cl)=C2)N=N1)N
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
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
Concentration Solvent Mass 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
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.

Select the appropriate dissolution method based on your experimental animal and administration route.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% 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 μL DMSO 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 μL DMSO 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.
Pureza y Documentación
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