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Cat. No.: HY-118569

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CP-115953

CP-115953 is an antitumor fluoroquinolone compound that targets eukaryotic topoisomerase II and Escherichia coli DNA gyrase. CP-115953 inhibits ATP hydrolysis and DNA relaxation by stimulating enzyme-mediated DNA cleavage, and enhances the expression of immune-related cytokines. CP-115953 is applicable for research on human cancers.

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CAS No.: 136440-70-5
Formule: C₁₉H₁₃F₂NO₄
Masse moléculaire:357.31

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

CP-115953 Chemical Structure

CAS No.: 136440-70-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

Topoisomerase II

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Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC50	6 μM	Cytotoxicity against wild-type Chinese hamster ovary cells assessed as reduction in cell survival via colony-forming cytotoxicity assay with 1 h treatment followed by 5 days incubation in fresh medium. Cytotoxicity against wild-type Chinese hamster ovary cells assessed as reduction in cell survival via colony-forming cytotoxicity assay with 1 h treatment followed by 5 days incubation in fresh medium.	8385484
CHO	EC50	9 μM	Cytotoxicity against wild-type Chinese hamster ovary (CHO) cells assessed via colony-forming assay. Cytotoxicity against wild-type Chinese hamster ovary (CHO) cells assessed via colony-forming assay.	9062121
CHO	EC50	12 μM	Cytotoxicity against Vpm^R-5 mutant Chinese hamster ovary (CHO) cells assessed via colony-forming assay. Cytotoxicity against Vpm^R-5 mutant Chinese hamster ovary (CHO) cells assessed via colony-forming assay.	9062121

In Vitro

CP-115953 (0.78-100 μM; 96 h) inhibits the proliferation of PHA-stimulated human peripheral blood lymphocytes, with an EC₅₀ of 3.1 μM after 96 h of incubation^[6].
CP-115953 (0.78-100 μM; 96 h) inhibits DNA synthesis in human peripheral blood lymphocytes stimulated by Phytohemagglutinin (PHA) (HY-N7038) in a dose-dependent manner^[6].

CP-115953 (0.78-100 μM; 48 h) stimulates IL-2 production in PHA-stimulated human peripheral blood lymphocytes in a dose-dependent manner^[6].
CP-115953 (6.25-50 μM; 48 h) modulates IFN-γ production and cytokine mRNA expression in PHA-stimulated human peripheral blood lymphocytes^[6].
CP-115953 (6 min) potently enhances Drosophila melanogaster topoisomerase II-mediated DNA cleavage, with an EC₂ of 5 μM^[3].
CP-115953 (up to 20 min) inhibits ATP hydrolysis catalyzed by Drosophila melanogaster topoisomerase II, with an IC₅₀ value of 110 μM^[3].
CP-115953 (50 μM; 6 min) exhibits DNA cleavage-enhancing activity against Drosophila melanogaster topoisomerase II^[3].
CP-115953 potently enhances calf thymus topoisomerase II-mediated DNA cleavage, with an EC₂ of 0.3 μM^[4].
CP-115953 (15 min) inhibits calf thymus topoisomerase II-mediated DNA relaxation, with an IC₅₀ of 3.2 μM^[4].
CP-115953 (50 μM) does not significantly inhibit the strand-passing DNA ligation mediated by purified Drosophila melanogaster topoisomerase II^[1].
CP-115953 (6 min) enhances the post-strand-passage double-stranded DNA cleavage mediated by purified Drosophila melanogaster topoisomerase II^[1].
CP-115953 (15 min) inhibits DNA relaxation mediated by purified Drosophila melanogaster topoisomerase II, with an IC₅₀ of approximately 50 μM^[1].
CP-115953 (50 μM; 6 min) increases the level of Drosophila melanogaster topoisomerase II-DNA cleavage complexes without inhibiting enzyme-mediated DNA ligation^[2].
CP-115953 (1 h) potently kills wild-type Chinese hamster ovary (CHO) cells, with an EC₅₀ of approximately 9 μM^[4].
CP-115953 (1 h) potently kills human A-431 squamous carcinoma cells, with an EC₅₀ of approximately 14 μM^[4].

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

Cell Viability Assay^[6]

Cell Line:

human peripheral blood lymphocytes
Concentration:

0.78, 1.6, 3.1, 6.2, 12.5, 25, 50, 100 μM
Incubation Time:

48, 72, 96 h
Result:

Inhibited DNA synthesis in human peripheral blood lymphocytes stimulated by Phytohemagglutinin (PHA).

Chemical Information

CAS No. 136440-70-5
Masse moléculaire 357.31
Formule C₁₉H₁₃F₂NO₄
SMILES

O=C(C1=CN(C2CC2)C3=C(C=C(F)C(C4=CC=C(O)C=C4)=C3F)C1=O)O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Robinson MJ, et al. Effects of quinolone derivatives on eukaryotic topoisomerase II. A novel mechanism for enhancement of enzyme-mediated DNA cleavage. J Biol Chem. 1991 Aug 5;266(22):14585-92. [Content Brief]

[2]. Robinson MJ, et al. Effects of novel fluoroquinolones on the catalytic activities of eukaryotic topoisomerase II: Influence of the C-8 fluorine group. Antimicrobial agents and chemotherapy. 1992 Apr;36(4):751-6.

[3]. Robinson MJ, et al. Effects of topoisomerase II-targeted drugs on enzyme-mediated DNA cleavage and ATP hydrolysis: evidence for distinct drug interaction domains on topoisomerase II. Biochemistry. 1993 Apr 13;32(14):3638-43.

[4]. Elsea SH, et al. Drug features that contribute to the activity of quinolones against mammalian topoisomerase II and cultured cells: correlation between enhancement of enzyme-mediated DNA cleavage in vitro and cytotoxic potential. Antimicrobial agents and chemotherapy. 1993 Oct;37(10):2179-86.

[5]. Elsea SH, et al. Quinolones share a common interaction domain on topoisomerase II with other DNA cleavage-enhancing antineoplastic drugs. Biochemistry. 1997 Mar 11;36(10):2919-24. [Content Brief]

[6]. Riesbeck K, et al. CP-115,953 stimulates cytokine production by lymphocytes. Antimicrob Agents Chemother. 1995 Feb;39(2):476-83.

[7]. Elsea SH, et al. A yeast type II topoisomerase selected for resistance to quinolones. Mutation of histidine 1012 to tyrosine confers resistance to nonintercalative drugs but hypersensitivity to ellipticine. J Biol Chem. 1995 Jan 27;270(4):1913-20.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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CP-115953

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