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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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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.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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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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