ARN-21934
Based on 1 Customer Validation
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.02%
- No. CAS: 2230854-93-8
- Fòrmula: C21H24N6
- Peso molecular:360.46
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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
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
topoisomerase II alpha |
topoisomerase II beta |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
12.6 μM
Compound: 14; ARN-21934
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Antiproliferation activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human A375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33079544] |
| A549 | IC50 |
17.1 μM
Compound: 14; ARN-21934
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Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33079544] |
| DU-145 | IC50 |
11.5 μM
Compound: 14; ARN-21934
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Antiproliferation activity against human DU145 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human DU145 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33079544] |
| G-361 | IC50 |
8.1 μM
Compound: 14; ARN-21934
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Antiproliferation activity against human G361 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human G361 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33079544] |
| HeLa | IC50 |
38.2 μM
Compound: 14; ARN-21934
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Antiproliferation activity against human Hela cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human Hela cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33079544] |
| MCF7 | IC50 |
15.8 μM
Compound: 14; ARN-21934
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Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33079544] |
In Vitro
ARN-21934 display a different affinity for topoIIα and topoIIβ. ARN-21934 is more potent against the α isoform, the IC50 value for the inhibition of DNA relaxation by topoIIα is 2 μM, the value for inhibition of DNA relaxation by topoIIβ is 120 μM[1].ARN-21934 exhibits a small panel of human cancer cell lines. It against melanoma (A375 and G-361), breast (MCF7), endometrial (HeLa), lung (A549), and androgen-independent prostate (DU145) cancer cells with IC50 values of 12.6 μM, 8.1 μM, 15.8 μM, 38.2 μM, 17.1 μM, and 11.5 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2230854-93-8
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Appearance Solid
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Peso molecular 360.46
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Fòrmula C21H24N6
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Color Light yellow to green yellow
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SMILES
NC1CC2=C(NC3=CC=C(N(C)C)C=C3)N=C(C4=CC=NC=C4)N=C2CC1
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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 : 8.33 mg/mL (23.11 mM; ultrasonic and warming and heat to 80°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 (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7742 mL | 13.8712 mL | 27.7423 mL | 69.3558 mL |
| 5 mM | 0.5548 mL | 2.7742 mL | 5.5485 mL | 13.8712 mL | |
| 10 mM | 0.2774 mL | 1.3871 mL | 2.7742 mL | 6.9356 mL | |
| 15 mM | 0.1849 mL | 0.9247 mL | 1.8495 mL | 4.6237 mL | |
| 20 mM | 0.1387 mL | 0.6936 mL | 1.3871 mL | 3.4678 mL |
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