Home DNA Damage/DNA Repair Topoisomerase inhibitor Hydroxy Camptothecine For research use only.

Hydroxy Camptothecine

Synonyms: 10-Hydroxycamptothecin, Hydroxycamptothecine

Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) 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.

Hydroxy Camptothecine Chemical Structure

Hydroxy Camptothecine Chemical Structure

CAS No. 64439-81-2

Purity & Quality Control

Hydroxy Camptothecine Related Products

Signaling Pathway

Topoisomerase Signaling Pathways

Topoisomerase Signaling Pathway

Biological Activity

Description Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) 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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models BALB/c-nude mice
Dosages 1, 2.5, 5, 7.5 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 364.35 Formula

C20H16N2O5
CAS No. 64439-81-2 SDF --
Smiles CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=CC5=C4)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 19 mg/mL ( (52.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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