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In vitro: GO-203 inhibits MUC1-C homodimerization which blocks its oncogenic function. Treatment of MUC1-overexpressing SKCO-1 and Colo-205 colon cancer cells with GO-203 is associated with downregulation of the TP53-inducible glycolysis and apoptosis regulator (TIGAR) protein. GO-203 regulates AKT-S6K1-elF4A signaling in colorectal cancer cells. Targeting MUC1-C with GO-203 inhibits p-AKT in colorectal cancer cells. GO-203 treatment also results in increases in reactive oxygen species (ROS) and loss of mitochondrial transmembrane potential.
In vivo: GO-203 is effective in inhibiting growth and survival of MUC1-positive colorectal cancer cells in mouse xenograft models. It is also effective in xenografts models of breast, prostate, lung and certain hematologic malignancy.
| Cell Experiment | |
|---|---|
| Cell lines | Human SW480 and LOVO colorectal cancer cells |
| Preparation method | To assess cell viability, 20,000–30,000 cells are plated and cultured for 48 h. GO-203 and CP-2 are added at 5 μM every day for six days. Cell viability is measured by trypan blue exclusion. |
| Concentrations | 5 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c nu/nu male/female mice with xenograft tumor |
| Formulation | PBS |
| Dosages | 18 mg/kg |
| Administration | i.p. |
| Molecular Weight | 2426.77 |
| Formula | C87H170N52O19S2.C2HF3O2 |
| CAS Number | 1222186-26-6 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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