Sunitinib is a multitargeted tyrosine kinase inhibitor of VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. It also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. The recommended dose of sunitinib is 50mg per day for 4 weeks followed by 2 weeks off-treatment (Schedule 4/2). Sunitinib demonstrated superior efficacy to interferon-α for the first-line treatment of mRCC. Sunitinib doubled progression-free survival compared with interferon-α; furthermore, median OS with sunitinib was greater than 2 years. Sunitinib has a distinct and predictable profile of adverse events, most of which are manageable with standard medical interventions. Evaluating the ability of Sunitinib (Sutent) to inhibit ligand-dependent receptor phosphorylation in cells, the effect of Sunitinib (Sutent) on ligand-dependent proliferation of cells was examined.
| Cell Experiment | |
|---|---|
| Cell lines | MV411 cells (FLT3-ITD) and OC1-AML5 cell lines |
| Preparation method | Cell lines were starved overnight in medium containing 0.1% FBS prior to addition of SU11248 and FL (50 ng/mL; FLT3-WT cells only). Proliferation was measured after 48 hours of culture using the Alamar Blue assay (Alamar Biosciences, Sacramento, CA) in triplicate for each condition, as described by the manufacturer. Trypan blue cell viability assays were performed in parallel and yielded similar results. |
| Concentrations | 0~10 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | MV4;11 or RS4;11 cells |
| Formulation | citrate-buffered solution (pH 3.5) |
| Dosages | 40, 20, 5 and 1 mg/kg/d |
| Administration | orally (PO) |
| Molecular Weight | 532.56 |
| Formula | C22H27FN4O2.C4H6O5 |
| CAS Number | 341031-54-7 |
| Solubility (25°C) | DMSO 15 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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| Oglufanide
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. |
| KLTWQELYQLKYKGI
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| Protein LMWP
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| CBO-P11
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. |
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