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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 |
| Related VEGFR/PDGFR Products |
|---|
| Conbercept
Conbercept (KH902) is a monoclonal antibody targeting VEGFRA fused to the IGHG1 Fc fragment. Conbercept is produced by the fusion of the second C-LIKE of FLT1 and the third and fourth C-LIKE of KDR with IGHG1 Fc. |
| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
| VEGFR-IN-1
VEGFR-IN-1 is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively. |
| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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