| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
ABCG2 (ATP binding cassette subfamily G member 2). Acridone treatment downregulates ABCG2 mRNA and protein expression. [1]
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|---|---|
| ln Vitro |
Acridone decreased the proliferation of MDA-MB-231 human breast cancer cells in a dose-dependent manner after 48 hours of treatment. At concentrations of 0.1, 0.5, and 1.0 μM, the optical density values were 0.714 ± 0.013, 0.498 ± 0.005, and 0.156 ± 0.011, respectively, compared to the control group (0.836 ± 0.009) (P < 0.05). [1]
In MDA-MB-231 cells, treatment with acridone at 0.5 and 1.0 μM significantly decreased the mRNA expression levels of ABCG2 compared to the control group (P < 0.05). No significant difference was observed at 0.1 μM. [1] In MDA-MB-231 cells, treatment with acridone at 0.1, 0.5, and 1.0 μM significantly decreased the protein expression levels of ABCG2 in a dose-dependent manner compared to the control group (P < 0.05). [1] |
| Cell Assay |
Cell culture: MDA-MB-231 cells were cultured in DMEM supplemented with 10% FBS and penicillin-streptomycin at 37°C in a 5% CO₂ incubator. [1]
Cell viability assay (MTT): Cells were seeded in 96-well plates at a density of 2.5 x 10³ cells/mL in 200 μL DMEM and cultured overnight. Cells were then treated with multiple concentrations of acridone (0.1, 0.5, and 1.0 μM) for 48 hours. 20 μL of MTT solution (5 mg/mL in PBS) was added to each well and incubated for 4 hours. The medium was then discarded, and 200 μL of DMSO was added to dissolve the formazan crystals. Optical density was measured at 570 nm. [1] RNA isolation and reverse transcription-quantitative PCR (RT-qPCR): MDA-MB-231 cells were treated with multiple concentrations of acridone (0.1, 0.5, and 1.0 μM) for 48 hours. Total RNA was isolated using TRIzol reagent. First-strand cDNA was prepared using a SYBR Green master kit. qPCR was performed using specific primers for ABCG2 and β-actin (as a control). The thermocycling conditions were: 95°C for 15 min, followed by 40 cycles of 95°C for 30 sec, 55°C for 30 min, and 72°C for 30 sec. Relative gene expression was calculated using the 2⁻ΔΔCq method. [1] Western blotting: MDA-MB-231 cells (2 x 10⁶ cells/dish) were treated with multiple concentrations of acridone (0.1, 0.5, and 1.0 μM) for 48 hours. Cell lysates were prepared using RIPA buffer containing protease and phosphatase inhibitors. Protein concentration was determined using the BCA assay. 30 μg of protein per lane were separated by 10% SDS-PAGE, transferred to PVDF membranes, blocked with 5% non-fat dry milk, and probed with an anti-ABCG2 antibody and a horseradish peroxidase-conjugated secondary antibody. Bands were visualized using an enhanced chemiluminescence system. [1] |
| References | |
| Additional Infomation |
Acridinones are acridinium compounds, specifically 9,10-dihydroacrylidine with an oxo group substituted at the 9-position. They are both acridinium compounds and cyclic ketones. Acridinones have been reported to exist in Thamnosma montana, and relevant data are available.
Acridone is a tricyclic acridine ring system. The acridine nucleus and its derivatives possess potent anticancer effects, as well as antibacterial, antimalarial, antiviral, anti-herpes, anti-allergy, and anti-leishmanial activities. [1] The study suggests that acridone may inhibit the proliferation of MDA-MB-231 human breast cancer cells, and this effect may be associated with the downregulation of ABCG2 expression. The findings indicate that acridone may be a potential candidate for the development of novel treatment strategies for human breast cancer. [1] |
| Molecular Formula |
C13H9NO
|
|---|---|
| Molecular Weight |
195.2167
|
| Exact Mass |
195.068
|
| CAS # |
578-95-0
|
| Related CAS # |
578-95-0;
|
| PubChem CID |
2015
|
| Appearance |
Light yellow to green yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
355.0±12.0 °C at 760 mmHg
|
| Melting Point |
>300 °C(lit.)
|
| Flash Point |
155.0±19.7 °C
|
| Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
| Index of Refraction |
1.642
|
| LogP |
2.57
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
15
|
| Complexity |
239
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C1C2=C([H])C([H])=C([H])C([H])=C2N([H])C2=C([H])C([H])=C([H])C([H])=C21
|
| InChi Key |
FZEYVTFCMJSGMP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H9NO/c15-13-9-5-1-3-7-11(9)14-12-8-4-2-6-10(12)13/h1-8H,(H,14,15)
|
| Chemical Name |
10H-acridin-9-one
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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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~128.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (12.81 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (12.81 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (12.81 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 | 5.1224 mL | 25.6121 mL | 51.2243 mL | |
| 5 mM | 1.0245 mL | 5.1224 mL | 10.2449 mL | |
| 10 mM | 0.5122 mL | 2.5612 mL | 5.1224 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06183229 | RECRUITING | Drug: Cycloferon Drug: Placebo |
Acute Respiratory Infection Influenza |
POLYSAN Scientific & Technological Pharmaceutical Company | 2023-09-15 | Phase 3 |
Products are for research use only; We do not sell to patients
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