product name (S)-10-Hydroxycamptothecin
Description: 10-Hydroxycamptothecin is a dose-dependent growth inhibitor of human microvascular endothelial cells (HMEC), and significantly inhibits the migration of HMEC with IC50 of 0.63 μM, resulting in a dose-dependent inhibition of tube formation with IC50 of 0.96 μM. The proliferation of human microvascular endothelial cells (HMEC) and seven human tumor cell lines were detected by SRB assay, resulting in study the antiangiogenic potential of 10-hydroxycamptothecin (HCPT), ,and the endothelial cell migration and tube formation were assessed using two in vitro model systems.
References: Oncol Rep. 2006 May;15(5):1273-9; Mol Pharmacol. 2000 Feb;57(2):243-51.
364.35
Formula
C20H16N2O5
CAS No.
19685-09-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 8 mg/mL (22.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL
Synonyms
10-HCPT
other peoduct :
| In Vitro |
In vitro activity: 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. 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. 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. Kinase Assay: Cell Assay: Cells (MDA-231, and BT-20 cells) are exposed to various concentrations of 10-Hydroxycamptothecin for 72 hours. Cell growth is monitored by the standard MTT assay. |
|---|---|
| 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%. 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. LD50: Mice 104mg/kg (i.p.). |
| Animal model | BALB/c-nu mice transplanted subcutaneously with Colo 205 cells |
| Formulation & Dosage | Dissolved in propylene glycol; 7.5 mg/kg; p.o. administration |
| References | Oncol Rep. 2006 May;15(5):1273-9; Mol Pharmacol. 2000 Feb;57(2):243-51. |
