2. Protein Tyrosine Kinase/RTK
  3. FLT3 c-Kit FGFR VEGFR PDGFR
  4. Dovitinib lactate

Dovitinib lactate  (Synonyms: CHIR-258 lactate; TKI-258 lactate)

Cat. No.: HY-10207 Purity: 99.75%
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Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.

For research use only. We do not sell to patients.

Dovitinib lactate Chemical Structure

Dovitinib lactate Chemical Structure

CAS No. : 692737-80-7

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 66 In-stock
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10 mg USD 96 In-stock
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Based on 10 publication(s) in Google Scholar

Other Forms of Dovitinib lactate:

Dovitinib lactate Related Antibodies

Top Publications Citing Use of Products

    Dovitinib lactate purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 May 7;8:287.  [Abstract]

    Determination in L3.6 cells of FGF2-induced FGFR phosphorylation by Western blot in the presence of Dovitinib. FGFR1 and alpha-Tubulin are used as loading controls.

    Dovitinib lactate purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

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    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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    PDGFR PDGFRβ PDGFRα

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively[1].

    IC50 & Target[1]

    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)

    In Vitro

    Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 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 IC50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively[1]. 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[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Dovitinib lactate Related Antibodies
    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[1]. 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[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    482.51

    Formula

    C24H27FN6O4
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (51.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
    References
    Cell Assay
    [2]

    To determine IC50 for SK-HEP1 cells, cells are plated at a density of 2×104 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. IC50 is calculated by nonlinear regression analysis using GraphPad Prism software[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    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)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0725 mL 10.3625 mL 20.7250 mL 51.8124 mL
    5 mM 0.4145 mL 2.0725 mL 4.1450 mL 10.3625 mL
    10 mM 0.2072 mL 1.0362 mL 2.0725 mL 5.1812 mL
    15 mM 0.1382 mL 0.6908 mL 1.3817 mL 3.4542 mL
    20 mM 0.1036 mL 0.5181 mL 1.0362 mL 2.5906 mL
    25 mM 0.0829 mL 0.4145 mL 0.8290 mL 2.0725 mL
    30 mM 0.0691 mL 0.3454 mL 0.6908 mL 1.7271 mL
    40 mM 0.0518 mL 0.2591 mL 0.5181 mL 1.2953 mL
    50 mM 0.0414 mL 0.2072 mL 0.4145 mL 1.0362 mL
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    Dovitinib lactate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Dovitinib692737-80-7CHIR-258TKI-258CHIR258CHIR 258TKI258TKI 258FLT3c-KitFGFRVEGFRPDGFRCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3SCFRCD117Fibroblast growth factor receptorVascular endothelial growth factor receptorPlatelet-derived growth factor receptorInhibitorinhibitorinhibit

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