TX-2552
Based on 1 Customer Validation
TX-2552 is an orally active tyrosine DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 value of 0.62 μM. TX-2552 can enhance the clastogenic activity of Topotecan (HY-13768) in mouse bone marrow cells, as well as the anti-tumor effect of Topotecan (HY-13768) in Krebs-2 ascites tumor mice.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 2446767-14-0
- Formula: C25H25FO3
- Molecular Weight:392.46
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
TDP1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chromosomal aberration mouse model[1].
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Dosage:20-160 mg/kg
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Administration:Oral gavage (p.o.) (Topotecan administered intraperitoneally at single doses of 0.25, 0.5, and 1 mg/kg induced chromosomal aberrations in bone marrow cells of F1(CBA×C57BL/6) hybrid mice in a dose-dependent manner)
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Result:Increased the level of aberrant metaphases induced by Topotecan (0.25 mg/kg) by 2.1-2.6 times.
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Animal Model:Krebs-2 ascites tumor female C57BL/6 mice model[2].
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Dosage:20-120 mg/kg
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Administration:Intraperitoneal injection (i.p.); once daily; 18 days (injected ascites cells intraperitoneally on day zero)
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Result:Reduced tumor volume and extended mouse lifespan.
Chemical Information
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CAS No. 2446767-14-0
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Appearance Solid
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Molecular Weight 392.46
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Formula C25H25FO3
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Color White to off-white
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SMILES
O=C(O1)C=C(C2=CC=C(F)C=C2)C3=C1C=C(OC/C=C(C)/CC/C=C(C)/C)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (63.70 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)
Purity & Documentation
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Data Sheet (271 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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Handling Instructions (2659 KB)
References
[1]. Zhanataev AK, et al. Enhancement of the Clastogenic Effects of Topotecan In Vivo by Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. Bull Exp Biol Med. 2024 May;177(1):30-34. [Content Brief]
[2]. Khomenko TM, et al. Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy. Int J Mol Sci. 2019 Dec 23;21(1):126. [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 | 2.5480 mL | 12.7402 mL | 25.4803 mL | 63.7008 mL |
| 5 mM | 0.5096 mL | 2.5480 mL | 5.0961 mL | 12.7402 mL | |
| 10 mM | 0.2548 mL | 1.2740 mL | 2.5480 mL | 6.3701 mL | |
| 15 mM | 0.1699 mL | 0.8493 mL | 1.6987 mL | 4.2467 mL | |
| 20 mM | 0.1274 mL | 0.6370 mL | 1.2740 mL | 3.1850 mL | |
| 25 mM | 0.1019 mL | 0.5096 mL | 1.0192 mL | 2.5480 mL | |
| 30 mM | 0.0849 mL | 0.4247 mL | 0.8493 mL | 2.1234 mL | |
| 40 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5925 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2740 mL | |
| 60 mM | 0.0425 mL | 0.2123 mL | 0.4247 mL | 1.0617 mL |