SU5416 (Semaxanib) is a potent and selective vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 inhibitor that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET. SU5416 inhibited cell migration of human vascular endothelial cells expressing both Flt-1 and KDR in response to VEGF and also inhibited the cell migration in response to placenta growth factor (PIGF), a specific ligand for Flt-1. Chemotaxis of monocytes expressing only Flt-1 was also inhibited by SU5416 in a dose-dependent manner. Moreover, SU5416 was found to inhibit tyrosine kinase of Flt-1 in response to PIGF in vitro. SU5416 efficiently inhibited Kit activity in vivo when administered on a twice-weekly schedule.
Another CAS# 194413-58-6
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Source | Int J Oncol (2015). Figure 3. SU5416 |
| Method | western blotting | |
| Cell Lines | endothelial cells (HUVEC) and 2H11 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | accumulation of cyclin B1 involved in the G2/M transition, whereas SU5416 alone reduced the expression of the regulator. In contrast, cyclin B1 expression was attenuated by 24 h of SU5416 treatment, regardless of the radiation dose. |
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Source | Int J Oncol (2015). Figure 2. SU5416 |
| Method | apoptosis assay | |
| Cell Lines | endothelial cells (HUVEC) and 2H11 cells | |
| Concentrations | 1 μmol/l | |
| Incubation Time | 48 h | |
| Results | Notably, 48 h of SU5416 and radiation exposure significantly increased the percentage of early apoptotic cells in endothelial cell lines. |
| Cell Experiment | |
|---|---|
| Cell lines | C6, Calu 6, A375, A431, and SF767T |
| Preparation method | Tumor Cell Lines and Growth Assays. The EPH4-VEGF cell line is a murine epithelial cell line engineered to overexpress murine VEGF. EPH4-VEGF cells were cultured in DMEM/F-12; C6 cells were cultured in Ham’s F-10 and A375, A431, and LNCAP cells in DMEM. All of these cultures were supplemented with 10% FBS and 2 mM L-glutamine. Calu 6 and SF767T cells were cultured in MEM supplemented with 10% FBS, 2 mM L-glutamine, 1 mM sodium pyruvate, and 0.1 mM MEM nonessential amino acids solution. C6, Calu 6, A375, A431, and SF767T were plated in their respective growth medium at 2 × 103 cells/100 μl/well in 96-well, flat-bottomed plates. SU5416 was serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth was measured after 96 h using the sulforhodamine B method. IC50s were calculated by curve fitting using four-parameter analysis. |
| Concentrations | 0, 0.05, 0.5, 5, 50 µm |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | Female BALB/c nu/nu mice Intracolonic Xenograft Model |
| Formulation | DMSO |
| Dosages | 25 mg/kg/day 50µl for 39 days |
| Administration | i.p. bolus injection |
| Molecular Weight | 238.28 |
| Formula | C15H14N2O |
| CAS Number | 204005-46-9 |
| Solubility (25°C) | DMSO 20 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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