| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
FLT3 1 nM (IC50) c-Kit 2 nM (IC50) FGFR1 8 nM (IC50) FGFR3 9 nM (IC50) VEGFR1 1 nM (IC50) VEGFR3 8 nM (IC50) VEGFR2 13 nM (IC50) PDGFRα 27 nM (IC50) PDGFRβ 210 nM (IC50)
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| ln Vitro |
At IC50 values of 25 nM, dovitinib potently suppresses the proliferation of FGF-stimulated B9 cells expressing F384L-FGFR3 as well as WT cells. Even at concentrations as high as 1 μM, B9-MINV cells exhibit resistance to the inhibitory action of dovitinib. Dovitinib has been shown to reduce the growth of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells. For KMS11 and OPM2, this means an IC50 of 90 nM and 550 nM, respectively[1]. When dovitinib is administered to SK-HEP1 cells, it causes G2/M cell cycle arrest, inhibits colony formation in soft agar, and blocks bFGF-induced cell migration. Dovitinib phosphorylates FGFR-1, FRS2-α, and ERK1/2 at their basal expression levels and in response to FGF[2].
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| ln Vivo |
In the KMS11-bearing mouse model, dovitinib (10 mg/kg, 30 mg/kg, 60 mg/kg, po) demonstrates a strong antitumor effect. The growth inhibition is 48%, 78.5%, and 94% in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment arms, respectively, in comparison to the mice receiving a placebo[1]. In HCC xenograft models, dovitinib exhibits strong anticancer and antimetastatic effects. Six HCC lines exhibit potent inhibition of tumor development by dovitinib. The inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways is correlated with the inhibition of angiogenesis development. In addition, dovitinib causes p-histone H2A-X and p27 to be upregulated, retinoblastoma to be dephosphorylated, p-cdk-2 and cyclin B1 to be downregulated, and cellular proliferation to be reduced as well as tumor cell apoptosis to be induced[2].
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| References |
[1]. Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948.
[2]. Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56(3), 595-601 |
| Molecular Formula |
C24H27FN6O4
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|---|---|
| Molecular Weight |
482.51
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| CAS # |
692737-80-7
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| Related CAS # |
Dovitinib;405169-16-6;Dovitinib dilactic acid;852433-84-2;Dovitinib lactate hydrate;915769-50-5
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| SMILES |
O=C(N1)C(C(NC2=C3)=NC2=CC=C3N4CCN(C)CC4)=C(N)C5=C1C=CC=C5F.O=C(O)C(C)O
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| Solubility (In Vitro) |
DMSO: ≥ 30 mg/mL (62.17 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0725 mL | 10.3625 mL | 20.7250 mL | |
| 5 mM | 0.4145 mL | 2.0725 mL | 4.1450 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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