TSU-68 (SU6668) is an oral tyrosine kinase inhibitor of VEGFR-2, PDGFR and FGFR. TSU-68 inhibits SCF-induced proliferation of MO7E cells with IC50 of 0.29 μM, and induces apoptosis. TSU-68 (SU6668) also inhibits Aurora kinases B and C (IC50 = 35 and 210 nM respectively). TSU68 suppresses tumor growth, blocks angiogenesis in tumors, and induces apoptosis of tumor vasculature and regression of established tumors. In a tumor model of HT29 human colon carcinoma, TSU-68 (200 mg/kg) decreases the average vessel permeability and average fractional plasma volume in the tumor rim and core.
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Source | Cell Physiol Biochem (2017). Figure 3. TSU-68 |
| Method | Measurement of VDCC currents | |
| Cell Lines | ASM cells | |
| Concentrations | 100-500 μM | |
| Incubation Time | 30 min | |
| Results | The currents were then removed by 316 μM TSU-68, while 100 μM TSU-68 partially blocked the currents |
| Cell Experiment | |
|---|---|
| Cell lines | HUVECs cells |
| Preparation method | HUVECs (seeded at 2 × 106 cells/10-cm plate) were grown to confluence in endothelial cell growth media [containing 12 μg/ml bovine brain extract, 10 μg/ml human epidermal growth factor, 1 μg/ml hydrocortisone, 2% (v/v) FBS, 50 μg/ml gentamicin, and 50 mg/ml amphotericin B in modified MCDB 131 (Clonetics Corp., Walkersville, MD)] and then quiesced in endothelial cell basal media (modified MCDB 131; Clonetics) containing 0.5% FBS for 24 h before drug treatment. All cell lines were incubated with the indicated concentrations of SU6668 for 60 min before ligand stimulation (100 ng/ml) for 10 min. Preparation of cell lysates, separation of cellular proteins (30 μg from NIH-3T3 engineered cells, 100 μg from HUVECs), and immunoblotting with antiphosphotyrosine antibody were performed as described previously. |
| Concentrations | 0~50 μM |
| Incubation time | 60 min |
| Animal Experiment | |
|---|---|
| Animal models | A375, Calu-6, A431, C6, and SF763T tumor cells xenograft in athymic mice |
| Formulation | DMSO |
| Dosages | 75 or 100 mg/kg |
| Administration | i.p. by bolus injection |
| Molecular Weight | 310.35 |
| Formula | C18H18N2O3 |
| CAS Number | 252916-29-3 |
| Solubility (25°C) | DMSO 28 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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