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  4. TX-2552

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.

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TX-2552 Chemical Structure

TX-2552 Chemical Structure

CAS No. : 2446767-14-0

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10 mg USD 255 In-stock
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Description

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[1][2].
IC50 & Target

TDP1[1].
In Vivo

TX-2552 (20-160 mg/kg; p.o.) can enhance the clastogenic effects of Topotecan (HY-13768) in mice with chromosomal abnormalities in bone marrow cells[1].
TX-2552 (20-120 mg/kg; once daily; 18 days; i.p.) can enhance the anti-tumor effect of topotecan (HY-13768) in Krebs-2 ascites tumor mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Chromosomal aberration mouse model[1].
Dosage: 20-160 mg/kg
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)
Result: Increased the level of aberrant metaphases induced by Topotecan (0.25 mg/kg) by 2.1-2.6 times.
Animal Model: Krebs-2 ascites tumor female C57BL/6 mice model[2].
Dosage: 20-120 mg/kg
Administration: Intraperitoneal injection (i.p.); once daily; 18 days (injected ascites cells intraperitoneally on day zero)
Result: Reduced tumor volume and extended mouse lifespan.
Molecular Weight

392.46

Formula

C25H25FO3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5480 mL 12.7402 mL 25.4803 mL
5 mM 0.5096 mL 2.5480 mL 5.0961 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TX-25522446767-14-0TX2552TX 2552OthersTopotecanchromosomemarrow cellsInhibitorinhibitorinhibit

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