(S)-10-Hydroxycamptothecin

Catalog No.S2423 Synonyms: 10-HCPT

For research use only.

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

(S)-10-Hydroxycamptothecin Chemical Structure

CAS No. 19685-09-7

Selleck's (S)-10-Hydroxycamptothecin has been cited by 6 Publications

Purity & Quality Control

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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

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]

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]

Protocol (from reference)

Cell Research:[2]
  • 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.
Animal Research:[4]
  • Animal Models: BALB/c-nu mice transplanted subcutaneously with Colo 205 cells
  • Dosages: ~7.5 mg/kg
  • Administration: Orally once per two days

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 364.35
Formula

C20H16N2O5

CAS No. 19685-09-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=CC5=C4)O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01963182 Completed Drug: Irinotecan First Line Metastatic Colorectal Cancer Centre Jean Perrin October 2013 Phase 2
NCT00520390 Completed Drug: EZN-2208 Lymphoma|Advanced Solid Tumors Enzon Pharmaceuticals Inc. May 2007 Phase 1
NCT00520637 Completed Drug: EZN-2208 Advanced Solid Tumors|Lymphoma Enzon Pharmaceuticals Inc. May 2007 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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