| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Atox1 and CCS (copper chaperones). Kd: Atox1 6.8 μM, CCS 8.2 μM.
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|---|---|
| ln Vitro |
In Canine Abrams, Canine D1, human HOS, and human MG63) cells, the IC50 values of DC_AC50 are 9.88 μM, 12.57 μM, 5.96 μM, and 6.68 μM, respectively[1]. Significant mitotic activity was seen in cells treated with DC_AC50 (0-10 μM). DC_AC50 (10 μM) decreased colony formation and increased OSA cells caused by carboplatin [1]. DC_AC50 at dosages of 3 μM and 10 μM. Canine and human OSA cells are inhibited in their migration by DC_AC50 (3 μM) [1]. DC_AC50 (2.5–10 μM) in a way that is depending on dosage. Adenocarcinoma cells (blank K562 cells, MDA-MB-231 breast cancer cells, H1299 human lung cancer cells, and 212LN head and neck cancer cells) are inhibited. Using human normal epithelial lung BEAS-2B or mammary gland cell MCF-10A as control cells, the DC_AC50 cell viability experiment was conducted [1].
DC_AC50 inhibits the copper chaperones Atox1 and CCS. By blocking copper trafficking, it disrupts copper-dependent processes in cells. This leads to increased copper and ROS levels, decreased COX activity and lipid biosynthesis, and ultimately inhibits cancer cell proliferation. |
| ln Vivo |
In vivo, DC_AC50 has been shown to significantly attenuate cancer cell proliferation and tumor growth. It is a potential therapeutic agent for cancers that are dependent on copper homeostasis.
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| Enzyme Assay |
DC_AC50 is evaluated in cell-free binding assays using purified Atox1 and CCS proteins. Fluorescence resonance energy transfer (FRET)-based assays or surface plasmon resonance (SPR) are used to measure binding affinity (Kd). The compound is incubated with the proteins, and binding is quantified.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Canine OSA (Abrams, D1 and human OSA (HOS, MG63) cells. Tested Concentrations: 0-10 μM. Incubation Duration: 72 h. Experimental Results: Dose-dependently diminished viability of OSA cells. Apoptosis analysis[1] Cell Types: Abrams and HOS cells. Tested Concentrations: 1, 3 and 10 μM (10 μM Carboplatin). Incubation Duration: 24 h. Experimental Results: Potentiated carboplatin-induced apoptosis. DC_AC50 is assessed in cell-based assays using various human cancer cell lines. Cells are treated with DC_AC50 (e.g., 10 μM), and cell proliferation is measured using MTT or other assays. Copper and ROS levels, COX activity, and lipid biosynthesis are also assessed. |
| Animal Protocol |
DC_AC50 is administered in animal models of cancer to evaluate its anti-tumor efficacy. Efficacy is assessed by measuring tumor growth inhibition and changes in copper homeostasis and ROS levels in tumor tissues. Pharmacokinetic studies are conducted to assess bioavailability and tissue distribution.
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| ADME/Pharmacokinetics |
No detailed PK data available. DC_AC50 has a molecular weight of 424.26.
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| Toxicity/Toxicokinetics |
No detailed toxicity data available. For research use only.
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| References |
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| Additional Infomation |
DC_AC50 is a dual inhibitor of Atox1 and CCS. Molecular formula: C17H12BrF2N3OS; MW: 424.26. For research use only.
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| Molecular Formula |
C17H12BRF2N3OS
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|---|---|
| Molecular Weight |
424.26
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| Exact Mass |
422.985
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| Elemental Analysis |
C, 48.13; H, 2.85; Br, 18.83; F, 8.96; N, 9.90; O, 3.77; S, 7.56
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| CAS # |
497061-48-0
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| PubChem CID |
1025330
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| Appearance |
White to off-white solid powder
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| LogP |
5.314
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
530
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1=C([H])C(=C([H])C(=C1N([H])C(C1=C(C2=C(N=C3C([H])([H])C([H])([H])C([H])([H])C3=C2[H])S1)N([H])[H])=O)F)F
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| InChi Key |
DFNOJNBNTVQPCA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12BrF2N3OS/c18-10-5-8(19)6-11(20)14(10)23-16(24)15-13(21)9-4-7-2-1-3-12(7)22-17(9)25-15/h4-6H,1-3,21H2,(H,23,24)
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| Chemical Name |
6-amino-N-(2-bromo-4,6-difluorophenyl)-4-thia-2-azatricyclo[7.3.0.03,7]dodeca-1,3(7),5,8-tetraene-5-carboxamide
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| Synonyms |
DCAC50; DC AC50; DC_AC50
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| HS Tariff Code |
2934.99.03.00
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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 : ~50 mg/mL (~117.85 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% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3570 mL | 11.7852 mL | 23.5705 mL | |
| 5 mM | 0.4714 mL | 2.3570 mL | 4.7141 mL | |
| 10 mM | 0.2357 mL | 1.1785 mL | 2.3570 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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