AD-8007
Based on 1 Customer Validation
AD-8007 is a blood-brain barrier-permeable ACSS2 inhibitor with human IC50 of 0.89 μM and Kd of 116.6 μM. AD-8007 reduces colony-forming ability, lipid storage levels and FASN protein expression, and induces cancer cell death. AD-8007 shrinks established tumors, acts synergistically with radiotherapy to inhibit tumor growth, reduces tumor burden, causes no obvious toxicity to normal brain tissue, and prolongs survival. AD-8007 exhibits superior metabolic stability. AD-8007 is applicable to research related to breast cancer brain metastasis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.36%
- No. CAS: 1497439-74-3
- Fòrmula: C22H26N2O
- Peso molecular:334.45
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
ACSS2 0.89 μM (IC50) |
ACSS2 116.6 μM (Kd) |
In Vitro
AD-8007 (0.6-150 μM; 60 min) potently and specifically inhibits human ACSS2 (but not hACSS1), with an IC50 of 0.89 μM for its ATPase inhibitory activity[1].
AD-8007 exhibits high metabolic stability in human liver microsomes, and shows moderate blood-brain barrier permeability without inhibiting P-glycoprotein in MDCK cell-based assays[1].
AD-8007 (100 μM; 48 h) reduces the clonogenic survival rate of MDA-MB-231BR and 4T1BR breast cancer brain metastasis cells and induces their cell death in vitro[1].
AD-8007 (20 μM; 6 days) inhibits the growth of established MDA-MB-231BR tumors in an ex vivo brain slice model without affecting the viability of normal brain tissue; its combination with 6 Gy radiotherapy synergistically blocks tumor growth[1].
AD-8007 (100 μM; 24-48 h) reduces acetyl-CoA levels, lipid droplet content, and FASN protein levels in MDA-MB-231BR and 4T1BR breast cancer brain metastatic cells in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AD-8007 (50 mg/kg; i.p.; daily; 14 days) reduces breast cancer brain metastasis tumor burden, decreases tumor proliferation, and extends survival in BalbC mice without significant weight loss[1].
AD-8007 (50 mg/kg; i.p.; single dose) penetrates the blood-brain barrier in BalbC mice, with significantly higher brain-to-blood levels than control compound VY-3-135[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nu/Nu (female, 4-6 weeks old, intracranial injection of luciferase-tagged MDA-MB-231BR breast cancer brain tropic cells)[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly reduced relative bioluminescence signal (tumor burden) compared to vehicle control.
Showed reduced tumor size and lower Ki-67 staining in brain sections compared to vehicle control.
Significantly extended mouse survival relative to vehicle control.
Caused no significant weight loss during treatment.
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Animal Model:BalbC (female, 4-6 weeks old, intracranial injection of luciferase-tagged 4T1BR breast cancer brain tropic cells)[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily
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Result:Significantly reduced tumor burden compared to vehicle control.
Decreased Ki-67 staining in tumors compared to vehicle control.
Extended mouse survival compared to vehicle control.
Caused no significant weight loss compared to vehicle control.
Chemical Information
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No. CAS 1497439-74-3
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Appearance Solid
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Peso molecular 334.45
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Fòrmula C22H26N2O
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Color White to off-white
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SMILES
O=C([C@@H](N)C1CC1)N2CC(C3=CC=CC=C3)(C4=CC=CC=C4)CCC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 16.67 mg/mL (49.84 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 2.9900 mL | 14.9499 mL | 29.8998 mL | 74.7496 mL |
| 5 mM | 0.5980 mL | 2.9900 mL | 5.9800 mL | 14.9499 mL | |
| 10 mM | 0.2990 mL | 1.4950 mL | 2.9900 mL | 7.4750 mL | |
| 15 mM | 0.1993 mL | 0.9967 mL | 1.9933 mL | 4.9833 mL | |
| 20 mM | 0.1495 mL | 0.7475 mL | 1.4950 mL | 3.7375 mL | |
| 25 mM | 0.1196 mL | 0.5980 mL | 1.1960 mL | 2.9900 mL | |
| 30 mM | 0.0997 mL | 0.4983 mL | 0.9967 mL | 2.4917 mL | |
| 40 mM | 0.0747 mL | 0.3737 mL | 0.7475 mL | 1.8687 mL |
AD-8007 Related Classifications
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