Determine the necessary mass, volume, or concentration for preparing a solution.
Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC 50 s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3 , c-Kit , FGFR1/3 , VEGFR1/2/3 and PDGFRα/β , respectively
In Vitro
Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC 50 values of 25 nM. B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. Dovitinib inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC 50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively. Treatment of SK-HEP1 cells with dovitinib results in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibits basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Dovitinib (10 mg/kg, 30 mg/kg, 60 mg/kg, p.o.) shows significant antitumor effect in the KMS11-bearing mice model, and the growth inhibition is 48%, 78.5%, and 94% in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment arms, respectively, compared with the placebo-treated mice . Dovitinib demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
To determine IC 50 for SK-HEP1 cells, cells are plated at a density of 2×10 4 cells per dish. After 48 h, cells are treated with 0, 0.01, 0.1, 1, 5, 10, 50, 100 μM dovitinib in DMEM containing 1% FBS for 24 h. Cell viability is determined with Cell Proliferation Assay. IC 50 is calculated by nonlinear regression analysis using GraphPad Prism software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Mice: Six HCC lines (06-0606, 26-0808A, 26-1004, 25-0705A, 5-1318, 21-0208) are used to establish tumors in male SCID mice. or dose-esponse experiments, mice bearing the 06-0606 xenografts re orally given vehicle (5% dextrose) or two doses of dovitinib (50 and 75 mg/kg) daily for 14 days. For time-dependent inhibition of dovitinib targets, mice bearing 06-0606 tumors are given orally 200 μL of either vehicle (n=6) or 50 mg/kg/day of dovitinib (n=10) . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:FLT3 1 nM (IC 50 ) c-Kit 2 nM (IC 50 ) FGFR1 8 nM (IC 50 ) FGFR3 9 nM (IC 50 ) VEGFR1 1 nM (IC 50 ) VEGFR3 8 nM (IC 50 ) VEGFR2 13 nM (IC 50 ) PDGFRα 27 nM (IC 50 ) PDGFRβ 210 nM (IC 50 )
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Clase | Diazinanes |
| Subclass | Piperazines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | N-arylpiperazines |
| Alternative Parents | Hydroquinolones Haloquinolines 4-aminoquinolines Hydroquinolines Benzimidazoles Dialkylarylamines Pyridinones N-methylpiperazines Aminopyridines and derivatives Benzenoids Aryl fluorides Alpha hydroxy acids and derivatives Vinylogous amides Imidazoles Heteroaromatic compounds Trialkylamines Secondary alcohols Lactams Monocarboxylic acids and derivatives Carboxylic acids Azacyclic compounds Primary amines Organopnictogen compounds Organofluorides Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Not available |
| Substituents | N-arylpiperazine - 4-aminoquinoline - Haloquinoline - Dihydroquinolone - Aminoquinoline - Quinoline - Dihydroquinoline - Benzimidazole - Dialkylarylamine - Tertiary aliphatic/aromatic amine - N-alkylpiperazine - N-methylpiperazine - Pyridinone - Aminopyridine - Benzenoid - Pyridine - Hydroxy acid - Aryl halide - Aryl fluoride - Alpha-hydroxy acid - Heteroaromatic compound - Vinylogous amide - Imidazole - Azole - Tertiary aliphatic amine - Tertiary amine - Secondary alcohol - Lactam - Azacycle - Monocarboxylic acid or derivatives - Carboxylic acid - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Primary amine - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Carbonyl group - Amine - Alcohol - Aromatic heteropolycyclic compound |
| Descripción | This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group. |
| External Descriptors | Not available |
| Solubilidad | DMSO : ≥ 30 mg/mL (62.17 mM) |
|---|---|
| Peso molecular | 482.500 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 3 |
| Exact Mass | 482.208 Da |
| Monoisotopic Mass | 482.208 Da |
| Topological Polar Surface Area | 148.000 Ų |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 737.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 1 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 2 |
Only protocols validated for the specific catalog item may be listed. None are provided for this entry.
General suggestion: When deploying as a pathway probe, include vehicle controls, concentration–response curves, and orthogonal validation (e.g., genetic perturbation). Verify compound integrity by LC–MS before critical studies.
Biological/biochemical context (literature, for research use only):
Caveats:
This compound is not a buffering agent and is not used to set or maintain pH. However, effective buffer handling is critical for its use in biochemical/cellular assays.
Practical guidance (general):
If precise aqueous solubility is required, determine experimentally under your exact buffer composition and temperature.
As a bioactive reference compound, dovitinib lactate does not have a “greener substitute” in the same sense as commodity solvents or reagents. However, greener practices can be applied to its handling and use.
Greener handling strategies (general):
Comparison (solvent perspective; general):
Note: Any change in solvent system can affect solubility and biological readouts; revalidate assay performance after adopting greener conditions.
For formulation and process research context only (no therapeutic claims):
Pharmacopeial/compendial status: Not specified for this item; refer to CoA/Spec Sheet. Any use is restricted to research applications; not for human or veterinary use.
Item-specific physicochemical specifications have not been provided for this catalog entry.
Practical notes (general):
Interpretation and context for this product category:
Recommendation: If your application is highly sensitive (e.g., quantitative kinase kinetics or LC–MS bioanalytical assay development), request the latest CoA and, where needed, a full analytical pack (chromatograms, spectra) for method suitability.
This product is primarily intended as a bioactive small‑molecule research tool rather than as a synthetic reagent. Accordingly, its value lies in biochemical and cellular studies rather than in promoting or participating in general organic reactions.
Research applications (general/literature context):
Practical tips:
Note: No synthetic or catalysis applications are typical for this compound; for reagent‑centric chemistry, consult other catalog sections (e.g., coupling reagents, bases, ligands).
Conventional “reaction conditions” (temperature, catalysts, yields) are not applicable: dovitinib lactate is a reference bioactive compound, not a reagent. The most relevant conditions pertain to solution preparation and biological assay use.
Stock/assay preparation (general literature practice):
Assay concentration ranges (general guidance):
These parameters are general; determine exact conditions experimentally for your system.
Safety information specific to this item has not been provided. Always consult the SDS for authoritative guidance.
For research use only. Not for human or veterinary use.
Dovitinib lactate is a heteroaromatic, basic small molecule salt. Practical dissolution and assay compatibility are the primary drivers for solvent choice.
Comparison (general guidance):
Always verify solubility, stability, and assay tolerance experimentally for your specific system.
Storage conditions (as provided):
Best practices (general, to complement the above):
Reconstitution (general guidance for bioactive small molecules):
Specifications not provided for this item (refer to CoA/Spec Sheet if needed):
For research use only. Not for human or veterinary use.
Dovitinib lactate is a small-molecule research compound supplied as the lactate salt of dovitinib (a multi-kinase inhibitor scaffold). For this catalog item, limited structure identifiers are provided.
Structural features (general/literature description):
Notes: Exact atom connectivity, stereochemistry (if any), and salt stoichiometry should be confirmed from the CoA/Spec Sheet for this specific lot.
This product is a finished bioactive small molecule and is not typically used as a building block or reagent in organic synthesis.
Context for medicinal chemistry (general):
If your goal is reagent‑centric synthesis (e.g., coupling chemistry, catalysis development), this compound is not an efficient choice; consult dedicated reagents and building blocks designed for synthetic transformations.
Only product‑data–verified target details may be listed here. For this catalog entry, no target or epitope information has been provided.
Note: Literature discusses dovitinib as a multi‑kinase inhibitor; however, item‑specific target data are not provided here by design. Consult primary references or perform in‑house profiling for your application.