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Dovitinib (TKI258) potently inhibited FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFRß and CSF-1R with IC50 values of 1, 2, 5, 10, 8, 27, 36 nM respectively. Dovitinib selectively blocked the growth of wild-type (WT) or activated mutant FGFR3-transformed B9 cells and human myeloma cell lines. Dovitinib was an effective treatment in a xenograft mouse model of FGFR3 multiple myeloma.
| Cell Experiment | |
|---|---|
| Cell lines | J807C, Y373C, K650E, G384D, wild type (WT), F384L and B9-MINV cells |
| Preparation method | Viability assay. Cell viability was assessed by 3-(4,5-dimethylthiazol)-2,5-diphenyl tetrazolium (MTT) dye absorbance according to the manufacturer's instructions (Boehringer Mannheim, Mannheim, Germany). Cells were seeded in 96-well plates at a density of 5000 (B9 cells) or 20 000 (MM cell lines) cells per well. Cells were incubated with 30 ng/mL aFGF and 100 μg/mL heparin or 1% IL-6 where indicated and increasing concentrations of CHIR-258. For each concentration of CHIR-258, 10-μL aliquots of drug or DMSO diluted in culture medium was added. For drug combination studies, cells were incubated with 0.5 μM dexamethasone, 100 nM CHIR-258, or both simultaneously where indicated. To evaluate the effect of CHIR-258 on growth of MM cells adherent to BMSCs, 10 000 KMS11 cells were cultured on BMSC-coated 96-well plates in the presence or absence of CHIR-258. Plates were incubated for 48 to 96 hours. |
| Concentrations | 0~400 n M |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | KMS11 cells xenograft mouse model |
| Formulation | 5 mM citrate buffer |
| Dosages | 10, 30, or 60 mg/kg daily for 21 days |
| Administration | oral gavage |
| Molecular Weight | 392.43 |
| Formula | C21H21FN6O |
| CAS Number | 405169-16-6 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
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| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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