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

Dovitinib lactate hydrate (Synonyms: TKI258 lactate hydrate; CHIR-258 lactate hydrate)

Cat. No.: HY-B0062
Handling Instructions

Dovitinib lactate hydrate (TKI258 lactate hydrate) 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 hydrate Chemical Structure

Dovitinib lactate hydrate Chemical Structure

CAS No. : 915769-50-5

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Top Publications Citing Use of Products

    Dovitinib lactate hydrate 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 hydrate 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 hydrate (TKI258 lactate hydrate) 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].

    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[1].

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

    Clinical Trial
    Molecular Weight

    500.52

    Formula

    C₂₄H₂₉FN₆O₅

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Product Name:
    Dovitinib lactate hydrate
    Cat. No.:
    HY-B0062
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