| CAS NO: | 19685-09-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 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; Hydroxycamptothecin; 10OHCPT; HCPT; 10hydroxycamptothecine; 10HCPT; 10 HCPT;
(S)10Hydroxycamptothecin; 10Hydroxy camptothecin; Hydroxycamptothecine; Camptothecin hydroxy10hydroxycamptothecin. |
| 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. 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. |
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