Hydroxy Camptothecine

Catalog No.S3898 Synonyms: 10-Hydroxycamptothecin, Hydroxycamptothecine

Hydroxy Camptothecine Chemical Structure

Molecular Weight(MW): 364.35

10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.

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Biological Activity

Description 10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
Targets
DNA topoisomerase I [1]
()
In vitro

10-HCPT has an inhibitory effect on phosphorylation of histone H1 and H3 in murine hepatoma cells and also exhibits a differentiation inducing effect in human HepG2 cells. 10-HCPT inhibits the cell growth, reduces the cell viability and disturbs the cell cycle distribution of human colon cancer cell line Colo 205. It induces cell cycle arrest in the G2/M phase[1].

In vivo 10-HCPT can be safely orally administered and, alternatively, a low-dose long-term treatment[1]. Prolonged elimination of HCPT in vivo may have a significant impact on its therapeutic effects. HCPT is metabolized to its carboxylate form and glucuronides. Dose-dependent toxicity is observed with i.v. administration of HCPT[2].

Protocol

Cell Research:[1]
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  • Cell lines: Colo 205 cells
  • Concentrations: 5, 10, 15 or 20 nM
  • Incubation Time: 24-120 h
  • Method: Colo 205 cells (5×105) (ATCC:CCL-222) are seeded in 25T flasks overnight and then treated without (control) and with 5, 10, 15 or 20 nM of HCPT, respectively. After treatment for 24-120 h, cells are harvested by trypsin-EDTA and then centrifuged at 1,500 rpm for 5 min at 4˚C. The cell pellet is resuspended in culture medium containing 0.04% trypan blue and the viable cells are enumerated by a hemocytometer.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: BALB/c-nude mice
  • Formulation: propylene glycol
  • Dosages: 1, 2.5, 5, 7.5 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 29 mg/mL (79.59 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 364.35
Formula

C20H16N2O5

CAS No. 64439-81-2
Storage powder
in solvent
Synonyms 10-Hydroxycamptothecin, Hydroxycamptothecine

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID