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

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

Cat. No.: HY-10207 Purity: 99.96%
Handling Instructions

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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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Dovitinib lactate:

Top Publications Citing Use of Products

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

    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.

    Dovitinib lactate purchased from MCE. Usage Cited in: Front Cell Dev Biol. 2020 May 7;8:287.

    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.

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    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].

    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].

    Clinical Trial
    Molecular Weight

    482.51

    Formula

    C₂₄H₂₇FN₆O₄

    CAS No.

    692737-80-7

    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
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (62.17 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2072 mL 1.0362 mL 2.0725 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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
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    Keywords:

    DovitinibCHIR-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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    Product Name:
    Dovitinib lactate
    Cat. No.:
    HY-10207
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