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Dovitinib

Cat. No. M1697
Dovitinib Structure
Synonym:

TKI258, CHIR-258

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 90 In stock
50mg USD 260 In stock
100mg USD 400 In stock
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Quality Control
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 392.43
Formula C21H21FN6O
CAS Number 405169-16-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

A validated tumorgraft model reveals activity of dovitinib against renal cell carcinoma.
Sivanand et al. Sci Transl Med. 2012 Jun 6;4(137):137ra75. PMID: 22674553.

Population Pharmacokinetic/Pharmacodynamic Modeling to Assist Dosing Schedule Selection for Dovitinib.
Wang et al. J Clin Pharmacol. 2012 Jan 27. PMID: 22287694.

Dovitinib sensitizes hepatocellular carcinoma cells to TRAIL and tigatuzumab, a novel anti-DR5 antibody, through SHP-1-dependent inhibition of STAT3.
Chen et al. Biochem Pharmacol. 2012 Mar 15;83(6):769-77. PMID: 22230479.

Dovitinib induces apoptosis and overcomes sorafenib resistance in hepatocellular carcinoma through SHP-1-mediated inhibition of STAT3.
Tai et al. Mol Cancer Ther. 2012 Feb;11(2):452-63. PMID: 22180308.

Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma.
Huynh et al. J Hepatol. 2012 Mar;56(3):595-601. PMID: 22027573.

Phase I/II and pharmacodynamic study of dovitinib (TKI258), an inhibitor of fibroblast growth factor receptors and VEGF receptors, in patients with advanced melanoma.
Kim et al. Clin Cancer Res. 2011 Dec 1;17(23):7451-61. PMID: 21976540.

CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma.
Trudel S, et al. Blood. 2005 Apr 1;105(7):2941-8. PMID: 15598814.

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Keywords: Dovitinib, TKI258, CHIR-258 supplier, VEGFR/PDGFR, inhibitors

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