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  2. Protein Tyrosine Kinase/RTK
  3. FLT3 TAM Receptor
  4. Gilteritinib hemifumarate

Gilteritinib hemifumarate  (Synonyms: ASP2215 hemifumarate)

目錄號: HY-12432A 純度: 99.75%
COA 產(chǎn)品使用指南 技術支持

Gilteritinib (ASP2215) hemifumarate 是一種有效的 ATP 競爭性的 FLT3/AXL 抑制劑，IC50 分別為 0.29 nM/0.73 nM。

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Gilteritinib hemifumarate Chemical Structure

Gilteritinib hemifumarate Chemical Structure

CAS No. : 1254053-84-3

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1344
In-stock
1 mg ￥434
In-stock
5 mg ￥1000
In-stock
10 mg ￥1500
In-stock
25 mg ￥2463
In-stock
50 mg ￥3500
In-stock
100 mg ￥5150
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Gilteritinib hemifumarate:

MCE 顧客使用本產(chǎn)品發(fā)表的 32 篇科研文獻

WB
Proliferation Assay

    Gilteritinib hemifumarate purchased from MCE. Usage Cited in: Cancer Cell Int. 2020 Jun 17;20:250.  [Abstract]

    Proliferation assay demonstrates that FLT3-ITD mutant cells (MV4-11 and MOLM13) are more sensitive to Gilteritinib compared with FLT3-WT cells (THP1 and HL60).

    Gilteritinib hemifumarate purchased from MCE. Usage Cited in: Cancer Cell Int. 2020 Jun 17;20:250.  [Abstract]

    MV4-11 and MOLM13 cells are treated with Gilteritinib (2.5 nM) and/or ATO (0.5 μM) for 48 h and protein levels of P-FLT3 and FLT3 are determined by Western blot. Gilteritinib exhibits a strong inhibition on the phosphorylated FLT3 even at a low concentration of 2.5 nM, but had little effect on total FLT3 and USP10.

    查看 TAM Receptor 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.

    IC50 & Target

    Axl

     

    體外研究
    (In Vitro)

    Of the 78 tyrosine kinases tested, Gilteritinib (ASP2215) inhibits FLT3, leukocyte tyrosine kinase (LTK), anaplastic lymphoma kinase (ALK), and AXL kinases by over 50% at 1 nM with an IC50 value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT[1]. Gilteritinib inhibits the activity of eight of the 78 tested kinases by over 50% at concentrations of either 1 nM (FLT3, LTK, ALK, and AXL) or 5 nM (TRKA, ROS, RET, and MER). The IC50s are 0.29 nM for FLT3 and 0.73 nM for AXL. Gilteritinib inhibits FLT3 at an IC50 that is approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). The antiproliferative activity of Gilteritinib is evaluated against MV4-11 and MOLM-13 cells, which endogenously express FLT3-ITD. After 5 days of treatment, Gilteritinib inhibits the growth of MV4-11 and MOLM-13 cells with mean IC50s of 0.92 nM (95% CI: 0.23-3.6 nM) and 2.9 nM (95% CI: 1.4-5.8 nM), respectively. Growth suppression of MV4-11 cells is accompanied by inhibition of FLT3 phosphorylation. Relative to vehicle control cells, phosphorylated FLT3 levels are 57%, 8%, and 1% after 2 h of treatment with 0.1 nM, 1 nM, and 10 nM Gilteritinib, respectively. In addition, doses as low as 0.1 nM or 1 nM result in the suppression of phosphorylated ERK, STAT5, and AKT, all of which are downstream targets of FLT3 activation. To investigate the effects of Gilteritinib on AXL inhibition, MV4-11 cells that expressed exogenous AXL are treated with Gilteritinib. At concentrations of 1 nM, 10 nM, and 100 nM for 4 h, Gilteritinib treatment decreases phosphorylated AXL levels by 38%, 29%, and 22%, respectively[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    In MV4-11 xenografted-mice, the concentration of Gilteritinib (ASP2215) in tumors is more than 20-fold higher than that in plasma with oral administration of Gilteritinib at 10 mg/kg for 4 days. Treatment of Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg. Further, Gilteritinib decreases tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells[1].

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

    610.75

    Formula

    C29H44N8O3 0.5C4H4O4
    CAS 號
    性狀

    固體

    顏色

    White to yellow

    運輸條件

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

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 6.67 mg/mL (10.92 mM; 超聲助溶 (<70°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    H2O 中的溶解度 : 2 mg/mL (3.27 mM; 超聲助溶)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.6373 mL 8.1867 mL 16.3733 mL
    5 mM 0.3275 mL 1.6373 mL 3.2747 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： Saline

      Solubility: 0.5 mg/mL (0.82 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (16.37 mM); 澄清溶液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    計算結果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.75%

    參考文獻
    Kinase Assay
    [2]

    The kinase inhibitory activity of Gilteritinib is tested against a panel of 78 tested kinases using ATP concentrations that are approximately equal to the Km value for each kinase in a TK-ELISA or off-chip mobility shift assay. Initially, two concentrations of Gilteritinib (1 nM and 5 nM) are tested to assess each compound’s inhibitory effect on TK activity. Further studies are then conducted using a dose range of Gilteritinib to determine IC50 values for kinases in which activity is inhibited by >50% with 1 nM Gilteritinib as well as for c-KIT. TK-ELISA and MSA assays are used to conduct IC50 studies for FLT3, LTK, AXL, and c-KIT; the HTRF KinEASE-TK assay is performed to assess the IC50 value of echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK)[2].

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

    The effect of Gilteritinib on MV4-11 and MOLM-13 cells is assessed using the CellTiter-Glo Luminescent Cell Viability Assay. Subsequent studies are conducted to examine the effect of Gilteritinib and Quizartinib on Ba/F3 cells expressing either FLT3-ITD, FLT3-D835Y, FLT3-ITD-D835Y, FLT3-ITD-F691 L, or FLT3-ITD-F691I. MV4-11 and MOLM-13 cells are treated with DMSO or increasing concentrations of Gilteritinib (0.01, 0.1, 1, 10, and 100 nM) for 5 days, and cell viability is measured using CellTiter-Glo[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Antitumor activity is evaluated in nude mice transplanted with MV4-11 AML cells. The pharmacokinetics in xenografted mice is also investigated. MV4-11 xenografted-mice are treated with oral administration of Gilteritinib at 10 mg/kg for 4 days. Treatment of Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg[1].

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

    Gilteritinib hemifumarate 相關分類

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.6373 mL 8.1867 mL 16.3733 mL 40.9333 mL
    DMSO 5 mM 0.3275 mL 1.6373 mL 3.2747 mL 8.1867 mL
    10 mM 0.1637 mL 0.8187 mL 1.6373 mL 4.0933 mL

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    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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    產(chǎn)品名稱：
    Gilteritinib hemifumarate
    目錄號：
    HY-12432A
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