Home DNA Damage/DNA Repair Topoisomerase inhibitor (S)-10-Hydroxycamptothecin For research use only.

(S)-10-Hydroxycamptothecin

Synonyms: 10-HCPT

(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.

(S)-10-Hydroxycamptothecin Chemical Structure

(S)-10-Hydroxycamptothecin Chemical Structure

CAS No. 19685-09-7

Purity & Quality Control

(S)-10-Hydroxycamptothecin Related Products

Signaling Pathway

Topoisomerase Signaling Pathways

Topoisomerase Signaling Pathway

Biological Activity

Description (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.
Targets
DNA topoisomerase I [1]
In vitro
In vitro 10-Hydroxycamptothecin inhibits the growth of BT-20 and MDA-231 cell with IC50 of 34.3 nM and 7.27 nM, respectively, more potently than camptothecin (CPT) with IC50 of >500 nM. 10-Hydroxycamptothecin potently induces human topoisomerase I-mediated cleavable complex formation of pBR322 plasmid DNA with EC50 of 0.35 μM, displaying >50-fold potency than CPT with EC50 of 18.85 μM. [2] 10-Hydroxycamptothecin treatment induces dose-dependent growth inhibition of human microvascular endothelial cells (HMEC) with IC50 of 0.31 μM, and significantly inhibits the migration of HMEC with IC50 of 0.63 μM. Treatment of HMEC cells with 10-Hydroxycamptothecin also results in a dose-dependent inhibition of tube formation with IC50 of 0.96 μM. [3] 10-Hydroxycamptothecin (5-20 nM) significantly inhibits the proliferation of Colo 205 cells, arrests the cells in the G2 phase of the cell cycle and induces apoptosis through a caspase-3-dependent pathway. [4]
Cell Research Cell lines MDA-231, and BT-20 cells
Concentrations Dissolved in DMSO, final concentrations ~50 μM
Incubation Time 72 hours
Method Cells are exposed to various concentrations of 10-Hydroxycamptothecin for 72 hours. Cell growth is monitored by the standard MTT assay.
In Vivo
In vivo 10-Hydroxycamptothecin treatment inhibits angiogenesis in a concentration-dependent fashion in the CAM model, with 95% inhibition at dose of 25 nM, more potently than suramin which at 125 nM inhibits angiogenesis only by 60%. [3] Oral administration of 10-Hydroxycamptothecin at low doses of 2.5-7.5 mg/kg every 2 days leads to significant growth inhibition of Colo 205 xenografts in mice without acute toxicity. [4] LD50: Mice 104mg/kg (i.p.). [5]
Animal Research Animal Models BALB/c-nu mice transplanted subcutaneously with Colo 205 cells
Dosages ~7.5 mg/kg
Administration Orally once per two days
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06143774 Recruiting
Advanced Solid Tumor
TaiRx Inc.
 October 31 2023 Phase 1
NCT04209595 Active not recruiting
Small Cell Lung Cancer|Extra-Pulmonary Small Cell Carcinomas
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 April 8 2020 Phase 1|Phase 2
NCT01963182 Completed
First Line Metastatic Colorectal Cancer
Centre Jean Perrin
 October 2013 Phase 2
NCT00520390 Completed
Lymphoma|Advanced Solid Tumors
Enzon Pharmaceuticals Inc.
 May 2007 Phase 1
NCT00520637 Completed
Advanced Solid Tumors|Lymphoma
Enzon Pharmaceuticals Inc.
 May 2007 Phase 1

Chemical Information & Solubility

Molecular Weight 364.35 Formula

C20H16N2O5
CAS No. 19685-09-7 SDF Download (S)-10-Hydroxycamptothecin 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 : 18 mg/mL ( (49.4 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 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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