(S)-10-Hydroxycamptothecin

BALB/c-nu mice transplanted subcutaneously with Colo 205 cells

Dissolved in DMSO, final concentrations ca.50 uM

ca.7.5 mg/kg

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 uM, displaying >50-fold potency than CPT with EC50 of 18.85 uM. [1] 10-Hydroxycamptothecin treatment induces dose-dependent growth inhibition of human microvascular endothelial cells (HMEC) with IC50 of 0.31 uM, and significantly inhibits the migration of HMEC with IC50 of 0.63 uM. Treatment of HMEC cells with 10-Hydroxycamptothecin also results in a dose-dependent inhibition of tube formation with IC50 of 0.96 uM. [2] 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. [3]

72 hours

364, 35

2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO