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Hydroxy Camptothecine Topoisomerase inhibitor

Cat.No.S3898

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 Topoisomerase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 364.35

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Quality Control

Batch: Purity: 99.69%
99.69

Solubility

In vitro
Batch:

DMSO : 19 mg/mL (52.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 364.35 Formula

C20H16N2O5

Storage (From the date of receipt)
CAS No. 64439-81-2 -- Storage of Stock Solutions

Synonyms 10-Hydroxycamptothecin, Hydroxycamptothecine Smiles CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=CC5=C4)O)O

Mechanism of Action

Targets/IC50/Ki
DNA topoisomerase I
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.
In vivo
10-HCPT can be safely orally administered and, alternatively, a low-dose long-term treatment. 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.
References

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