AD-5584
Based on 1 Customer Validation
AD-5584 is a selective and blood-brain barrier-penetrant ACSS2 inhibitor (IC50 = 0.86 μM). AD-5584 binds to the nucleotide-binding pocket of ACSS2, blocking CoA binding and acetyl transfer through steric hindrance, thereby inhibiting the conversion of acetate to acetyl-CoA. AD-5584 decreases acetyl-CoA levels, lipid droplet content, FASN expression, E2F1, SLC7A11, and GPX4 levels, and reduces E2F1 occupancy at the SLC7A11 promoter. AD-5584 induces ferroptosis, lipid peroxidation, malondialdehyde accumulation, and cell death, and decreases clonogenic survival and proliferative capacity. AD-5584 can be used for research on breast cancer brain metastasis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.86%
- CAS 番号: 2306525-79-9
- 分子式: C22H24ClFN4O
- 分子量:414.90
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
ACSS2 0.86 μM (IC50) |
GPX4 |
体外実験
AD-5584 (100 μM; 48 h) significantly reduces lipid droplet content in MDA-MB-231BR breast cancer brain metastatic cells[1].
AD-5584 (100 μM; 24 h) reduces FASN protein levels in MDA-MB-231BR breast cancer brain metastatic cells[1].
AD-5584 (100 μM; 48 h) induces ferroptotic cell death in MDA-MB-231-BR cells, which is blocked by ferrostatin-1[2].
AD-5584 (100 μM; 48 h) induces lipid peroxidation in MDA-MB-231-BR cells, which is blocked by ferrostatin-1[2].
AD-5584 (100 μM; 48 h) E2F1 overexpression protects MDA-MB-231-BR cells from AD-5584-induced cell death and lipid peroxidation[2].
AD-5584 (100 μM; 48 h) reduces E2F1, SLC7A11, and GPX4 protein levels in 4T1-BR cells[2].
AD-5584 (100 μM; 48 h) induces ferroptotic cell death in 4T1-BR cells, which is blocked by Ferrostatin-1 (HY-100579) [2].
AD-5584 (100 μM; 48 h) induces lipid peroxidation in 4T1-BR cells, which is blocked by Ferrostatin-1 (HY-100579)[2].
AD-5584 induces ferroptosis-mediated tumor regression of MDA-MB-231-BR cells in ex vivo brain slices, with no observable toxicity to normal brain tissue[2].
AD-5584 induces ferroptosis-mediated tumor regression of 4T1-BR cells in ex vivo brain slices[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231BR breast cancer brain metastatic cells
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Concentration:100 μM
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Incubation Time:48 h (treatment); 15 min (staining)
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Result:Significantly reduced lipid droplet content compared to control.
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Cell Line:MDA-MB-231BR breast cancer brain metastatic cells
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Concentration:100 μM
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Incubation Time:24 h
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Result:Reduced protein levels of FASN compared to DMSO control.
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Cell Line:MDA-MB-231-BR human breast cancer brain metastatic cells
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Concentration:100 μM
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Incubation Time:48 h
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Result:Reduced E2F1, SLC7A11, and GPX4 protein levels compared to control-treated cells.
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Cell Line:MDA-MB-231-BR human breast cancer brain metastatic cells
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Concentration:100 μM
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Incubation Time:48 h
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Result:Significantly increased cell death compared to control-treated cells.
Reversed the increase in cell death by co-treatment with Ferrostatin-1.
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Cell Line:4T1-BR mouse breast cancer brain metastatic cells
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Concentration:100 μM
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Incubation Time:48 h
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Result:Reduced E2F1, SLC7A11, and GPX4 protein levels compared to control-treated cells.
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Cell Line:4T1-BR mouse breast cancer brain metastatic cells
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Concentration:100 μM
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Incubation Time:48 h
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Result:Significantly increased cell death compared to control-treated cells.
Reversed the increase in cell death by co-treatment with Ferrostatin-1.
体内実験
AD-5584 (systemic; 14 days) inhibits breast cancer brain metastasis growth in immunocompromised mice bearing intracranial MDA-MB-231-BR tumors[2].
AD-5584 (50 mg/kg; i.p.; daily; 10 days) suppresses breast cancer brain metastatic growth and extends survival in mouse intracranial models[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nu/Nu athymic nude mice (4-6 weeks old; female for MFP model) injected with f MDA-
MB-231 or MDA-MB-231-BR cells[3] -
Dosage:50 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Significantly blocked breast cancer brain metastatic growth of both 4T1-BR and MDA-MB-231-BR cells in vivo.
Significantly extended survival of treated mice compared to control.
No weight loss or observable behavioral changes were detected in treated animals.
化学情報
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CAS 番号 2306525-79-9
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性状 Solid
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分子量 414.90
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分子式 C22H24ClFN4O
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Color White to off-white
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SMILES
FC1=CC=C(C(N2CCCCC2)C(N(C)CC3=NC4=CC(Cl)=CC=C4N3)=O)C=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 12.5 mg/mL (30.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (299 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4102 mL | 12.0511 mL | 24.1022 mL | 60.2555 mL |
| 5 mM | 0.4820 mL | 2.4102 mL | 4.8204 mL | 12.0511 mL | |
| 10 mM | 0.2410 mL | 1.2051 mL | 2.4102 mL | 6.0255 mL | |
| 15 mM | 0.1607 mL | 0.8034 mL | 1.6068 mL | 4.0170 mL | |
| 20 mM | 0.1205 mL | 0.6026 mL | 1.2051 mL | 3.0128 mL | |
| 25 mM | 0.0964 mL | 0.4820 mL | 0.9641 mL | 2.4102 mL | |
| 30 mM | 0.0803 mL | 0.4017 mL | 0.8034 mL | 2.0085 mL |
AD-5584 関連分類
HY-161116 関連分類
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