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

Dovitinib lactate  (Synonyms: 多韦替尼乳酸盐; CHIR-258 lactate; TKI-258 lactate)

目录号: HY-10207 纯度: 99.62%
COA 产品使用指南

摩尔计算器

Dovitinib lactate (TKI258 lactate) 是多靶点的酪氨酸激酶抑制剂，抑制 FLT3，c-Kit，FGFR1/3，VEGFR1/2/3 和 PDGFRα/β 的 IC50 值分别为 1，2，8/9，10/13/8，27/210 nM。

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Dovitinib lactate Chemical Structure

Dovitinib lactate Chemical Structure

CAS No. : 692737-80-7

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605
In-stock
5 mg ￥550
In-stock
10 mg ￥880
In-stock
50 mg ￥2650
In-stock
100 mg ￥4400
In-stock
200 mg ￥7700
In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Dovitinib lactate:

Dovitinib lactate 相关抗体

Top Publications Citing Use of Products

    Dovitinib lactate 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 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.

    查看 FGFR 亚型特异性产品:

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    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    查看 VEGFR 亚型特异性产品:

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

    查看 PDGFR 亚型特异性产品:

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    PDGFR PDGFRβ PDGFRα

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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)

    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]. 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].

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

    Dovitinib lactate 相关抗体:
    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]. 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].

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

    482.51

    Formula

    C24H27FN6O4
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    多韦替尼乳酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

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

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 25 mg/mL (51.81 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献
    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.
    参考文献

    Dovitinib lactate 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 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
    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-258多韦替尼乳酸盐CHIR258CHIR 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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    目录号：
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