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

Gilteritinib  (Synonyms: 吉瑞替尼; 吉列替尼; ASP2215)

目录号: HY-12432 纯度: 99.34%
COA 产品使用指南

摩尔计算器

Gilteritinib (ASP2215) 是一种有效的 ATP 竞争性的 FLT3/AXL 抑制剂，IC50 分别为 0.29 nM/0.73 nM。

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Gilteritinib Chemical Structure

Gilteritinib Chemical Structure

CAS No. : 1254053-43-4

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Customer Review

Other Forms of Gilteritinib:

Gilteritinib 相关抗体

Top Publications Citing Use of Products
WB
Proliferation Assay

    Gilteritinib 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 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.

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    Axl Mer Tyro3

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.

    IC50 & Target

    Axl

     

    体外研究
    (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.

    Gilteritinib 相关抗体:
    体内研究
    (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

    552.71

    Formula

    C29H44N8O3
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

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

    4°C, stored under nitrogen

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

    溶解性数据
    细胞实验： 

    Ethanol 中的溶解度 : 100 mg/mL (180.93 mM; 超声助溶; 酸性条件溶解 (HCL 调节，pH≈2))

    DMSO 中的溶解度 : 2 mg/mL (3.62 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 1.8093 mL 9.0463 mL 18.0927 mL
    5 mM 0.3619 mL 1.8093 mL 3.6185 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 (stored under nitrogen)。-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

    动物实验：

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (18.09 mM); 悬浊液; 超声助溶

    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

    纯度: 99.69%

    COA (264 KB) LCMS (96 KB)

    产品使用指南 (1538 KB)
    参考文献
    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.
    参考文献

    Gilteritinib 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 (stored under nitrogen)。-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 / Ethanol 1 mM 1.8093 mL 9.0463 mL 18.0927 mL 45.2317 mL
    Ethanol 5 mM 0.3619 mL 1.8093 mL 3.6185 mL 9.0463 mL
    10 mM 0.1809 mL 0.9046 mL 1.8093 mL 4.5232 mL
    15 mM 0.1206 mL 0.6031 mL 1.2062 mL 3.0154 mL
    20 mM 0.0905 mL 0.4523 mL 0.9046 mL 2.2616 mL
    25 mM 0.0724 mL 0.3619 mL 0.7237 mL 1.8093 mL
    30 mM 0.0603 mL 0.3015 mL 0.6031 mL 1.5077 mL
    40 mM 0.0452 mL 0.2262 mL 0.4523 mL 1.1308 mL
    50 mM 0.0362 mL 0.1809 mL 0.3619 mL 0.9046 mL
    60 mM 0.0302 mL 0.1508 mL 0.3015 mL 0.7539 mL
    80 mM 0.0226 mL 0.1131 mL 0.2262 mL 0.5654 mL
    100 mM 0.0181 mL 0.0905 mL 0.1809 mL 0.4523 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:

    Gilteritinib1254053-43-4ASP2215ASP 2215ASP-2215FLT3TAM ReceptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Tyro3AxlMerInhibitorinhibitorinhibit

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