Pyrazoloacridine
Based on 1 Customer Validation
Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
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- Pureza: 98.05%
- No. CAS: 99009-20-8
- Fòrmula: C19H21N5O3
- Peso molecular:367.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Ver todos los productos específicos de isoformas Topoisomerase
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-8 | IC50 |
0.136 μM
Compound: 15
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Growth inhibition against human colon carcinoma HCT-8 cell line
Growth inhibition against human colon carcinoma HCT-8 cell line
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[PMID: 8280289] |
| L1210 | IC50 |
0.424 μM
Compound: 15
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Growth inhibition against mouse leukemia L1210 cell line
Growth inhibition against mouse leukemia L1210 cell line
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[PMID: 8280289] |
| L1210 | IC50 |
0.424 μM
Compound: 9-methoxypyrazoloacridine (PZA)
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In vitro cytotoxicity against murine leukemia cell line L1210
In vitro cytotoxicity against murine leukemia cell line L1210
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[PMID: 16169719] |
Pyrazoloacridine (NSC 366140, PD 115934) exhibits IC50 values of 10.7 μM and 4.5 μM for oxic and hypoxic HCT-8 cells[1].
Pyrazoloacridine (NSC 366140, 2-4 μM) abolishes the catalytic activity of both topo I and topo II in vitro[2].
Pyrazoloacridine (NSC 366140) displays activity against cisplatin- and paclitaxel-resistant ovarian cancer[2].
Pyrazoloacridine (NSC 366140) has been shown to cause delayed DNA fragmentation in MCF-7 breast cancer cells[2].
Pyrazoloacridine (NSC 366140) induces apoptosis in P53-deficient Hep 3B human hepatoma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 Myeloid Leukemia Cells.
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Concentration:0-500 μM.
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Incubation Time:1 h or 24 h.
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Result:When K562 cells were incubated with PA for 1 h and then plated in soft agar, an IC50 of -50 μM was observed. In contrast, when cells were incubated for 24 h with PA, the IC50 was 1.25 μM.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 99009-20-8
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Appearance Solid
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Peso molecular 367.40
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Fòrmula C19H21N5O3
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Color Light brown to orange
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SMILES
O=[N+](C1=CC=C2C3=C1NC4=CC=C(OC)C=C4C3=NN2CCCN(C)C)[O-]
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Synonyms
NSC 366140; PD 115934
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 16.67 mg/mL (45.37 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 (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. J S Sebolt, et al. Pyrazoloacridines, a new class of anticancer agents with selectivity against solid tumors in vitro. Cancer Res. 1987 Aug 15;47(16):4299-304. [Content Brief]
[2]. A A Adjei, et al. Effect of pyrazoloacridine (NSC 366140) on DNA topoisomerases I and II. Clin Cancer Res. 1998 Mar;4(3):683-91. [Content Brief]
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 | 2.7218 mL | 13.6091 mL | 27.2183 mL | 68.0457 mL |
| 5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL | 13.6091 mL | |
| 10 mM | 0.2722 mL | 1.3609 mL | 2.7218 mL | 6.8046 mL | |
| 15 mM | 0.1815 mL | 0.9073 mL | 1.8146 mL | 4.5364 mL | |
| 20 mM | 0.1361 mL | 0.6805 mL | 1.3609 mL | 3.4023 mL | |
| 25 mM | 0.1089 mL | 0.5444 mL | 1.0887 mL | 2.7218 mL | |
| 30 mM | 0.0907 mL | 0.4536 mL | 0.9073 mL | 2.2682 mL | |
| 40 mM | 0.0680 mL | 0.3402 mL | 0.6805 mL | 1.7011 mL |
Pyrazoloacridine Related Classifications
HY-108969 Related Classifications
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