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)

目录号: HY-B0062
产品使用指南

Dovitinib lactate hydrate (TKI258 lactate hydrate) 是多靶点的酪氨酸激酶抑制剂,抑制 FLT3c-KitFGFR1/3VEGFR1/2/3PDGFRα/βIC50 值分别为 1,2,8/9,10/13/8,27/210 nM。

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Dovitinib lactate hydrate Chemical Structure

Dovitinib lactate hydrate Chemical Structure

CAS No. : 915769-50-5

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Dovitinib lactate hydrate 的其他形式现货产品:

Customer Review

Other Forms of Dovitinib lactate hydrate:

    Dovitinib lactate hydrate purchased from MCE. 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 hydrate purchased from MCE. 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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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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)

    体外研究
    (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.

    体内研究
    (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
    分子量

    500.52

    Formula

    C24H29FN6O5

    CAS 号
    中文名称

    多韦替尼乳酸盐水合物

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

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

    纯度 & 产品资料
    参考文献
    • 摩尔计算器

    • 稀释计算器

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    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.

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    产品名称:
    Dovitinib lactate hydrate
    目录号:
    HY-B0062
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