SU11274 (PKI-SU11274) is a Met kinase inhibitor with IC50 of 10 nM. c-Met is a prognostic marker and potential therapeutic target in clear cell renal cell carcinoma. c-Met protein was activated in all cell lines, and SU11274 can block proliferation (and colony formation). c-Met inhibition could significantly suppress cell survival and proliferation as well as enhance the radiosensitivity of DU145 cells. SU11274 on DU145 cells may include the inhibition of c-Met signaling, depolarization of the mitochondrial membrane potential, impairment of DNA repair function, abrogation of cell cycle arrest, and enhancement of cell death.
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Source | Oncol Lett (2015). Figure 5.SU11274 |
| Method | Scratch assay | |
| Cell Lines | PK-45H cells | |
| Concentrations | 30 μM | |
| Incubation Time | 48 h | |
| Results | Following treatment with 30 μM SU11274, cell motility was suppressed to 1.0±0.3% in MIA‑Paca2 cells (P<0.05) and 14.7±3.5% in PK‑45H cells (P<0.05) of the level of cells treated with 0 μM SU11274, respectively. |
| Cell Experiment | |
|---|---|
| Cell lines | LoVo cells line |
| Preparation method | MTT assay. After pancreatic enzymeization, cells were seeded in 96-well plates at 1 9 105/ml (200 ll/well) and allowed to adhere overnight. SU11274, dissolved in 1 % DMSO and diluted in medium, was added at different concentrations 0.1, 0.5, 2.5 μM, 2μl per well. Another 4 wells were set as a reference and incubated for 24, 48 and 72 h. Twenty microliter MTT (5 g/l; Invitrogen, USA) was added, and cells were incubated for another 4 h. The supernatant was removed, 150 ll DMSO was added and oscillated for 10 min avoiding light at room temperature. The assessment procedure was repeated 3 times, and the average value was determined from each well as the absorbance value at 490 nm on a microplate reader. |
| Concentrations | 0.1, 0.5, 2.5 μM |
| Incubation time | 24, 48 and 72 h |
| Animal Experiment | |
|---|---|
| Animal models | LoVo cells tumor xenograft in 4- to 5-week-old female nude mice (BALB/c-nu/nu) |
| Formulation | 1 % DMSO |
| Dosages | 0.18, 0.09, 0.0225 mg/kg once daily for 30 days from the day that the tumors became palpable |
| Administration | celiac injection |
| Molecular Weight | 568.09 |
| Formula | C28H30ClN5O4S |
| CAS Number | 658084-23-2 |
| Solubility (25°C) | DMSO 82 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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