Description
FK-3000 is a potent anti-tumor agent that inhibits the growth of carcinoma cells through apoptosis and induction cell cycle arrest. FK-3000 also exhibit antiviral effects against HSV-1 and HIV-1.
Structural Formula
FK-3000
Source
Plants >Menispermaceae > Stephania delavayiDiels
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
COC1=C([C@]([H])(C2)NCC3)[C@]3(C4=C2C=CC(OC)=C4OC(C)=O)C[C@H](OC(C)=O)[C@@H]1O
In Vivo
FK-3000 (1 mg/kg/day; i.p. daily for 24 d) inhibits tumor growth and shows no signs of toxicity in an MDA-MB-231 xenografted mouse model.FK-3000 (10-25 mg/kg; p.o. for 10 d) significantly delays skin lesion, limits the development of further lesions and prolongs the mean survival time of HSV-1 infected mice.
In Vitro
FK-3000 (0-5 μg/mL; 48 h) inhibits cell proliferation, with IC50s of 0.52, 0.77, 0.22, 2.70, 0.40, and 1.90 μg/mL for MDA-MB-231, MCF-7, PC-3, A-431, HT-29, and CT-26 cells, respectively.FK-3000 (0.5-5.0 μg/mL; 24-48 h) induces MDA-MB-231 cell apoptosis in a dose- and time-dependent manner. FK-3000 (0.5-5.0 μg/mL; 24-48 h) induces G2/M phase arrest in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner. FK-3000 (0.5-5.0 μg/mL; 60-120 min or 24-48 h) reduces NF-κB phosphorylation levels and COX-2 expression in MDA-MB-231 cells.FK-3000 (5.0 μg/mL; 120 min) effectively blocks NF-κB translocation from cytoplasm to nucleus in MDA-MB-231 cells.