2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor
  4. Merestinib dihydrochloride

Merestinib dihydrochloride  (Synonyms: LY2801653 dihydrochloride)

目录号: HY-15514A 纯度: 99.36%
COA 产品使用指南

摩尔计算器

Merestinib dihydrochloride (LY2801653 dihydrochloride) 是一种有效的口服生物可利用的具有抗肿瘤活性的 c-Met 抑制剂 (Ki=2 nM)。Merestinib dihydrochloride 对 MST1R (IC50=11 nM)、FLT3 (IC50=7 nM)、AXL (IC50=2 nM)、MERTK (IC50=10 nM)、TEK (IC50=63 nM)、ROS1、DDR1/2 (IC50=0.1/7 nM) 和 MKNK1/2 (IC50=7 nM) 也有较强的活性。

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Merestinib dihydrochloride Chemical Structure

Merestinib dihydrochloride Chemical Structure

CAS No. : 1206801-37-7

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Other Forms of Merestinib dihydrochloride:

Merestinib dihydrochloride 相关抗体

Top Publications Citing Use of Products

    Merestinib dihydrochloride purchased from MCE. Usage Cited in: Cancer Discov. 2016 Dec;6(12):1334-1341.  [Abstract]

    The MET D1228V mutation renders all type I MET inhibitors ineffective, as evidence by the failure of Savolitinib, PF-02341066, and INC280 to inhibit MET phosphorylation. In contrast, type II MET inhibitors XL184, MGCD265, and Merestinib (LY2801653) are able to effectively suppress MET phosphorylation in the presence of the D1228V mutation.

    查看 Discoidin Domain Receptor 亚型特异性产品:

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    DDR1 DDR2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM)[1][2].

    IC50 & Target

    Ki: 2 nM (c-Met)[1]
    IC50: 11 nM (MST1R), 7 nM (FLT3), 2 nM (AXL), 10 nM (MERTK), 63 nM (TEK), 0.1/7 nM (DDR1/2), 7 nM (MKNK1/2)[1]
    体外研究
    (In Vitro)

    Merestinib (LY2801653) also inhibits MST1R (IC50=11 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TYRO3 (IC50=28 nM), ROS1, PDGFRA (IC50=41 nM), FLT3 (IC50=7 nM), TEK (IC50=63 nM), DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM)[1].
    Merestinib demonstrates effects on MET pathway-dependent cell scattering and cell proliferation. The mean IC50 value (n=6 determinations) of Merestinib for inhibition of MET auto-phosphorylation in HGF-stimulated H460 cells is 35.2±6.9 nM and the IC50 for MET auto-phosphorylation in S114 cells is 59.2 nM. Transfection with the MET variants confers growth-factor independence and treatment with Merestinib inhibits growth of these MET variant clones with an IC50 ranging from 3-fold more potent (V1092I) to approximately 6-fold less potent (L1195V) compare with the growth inhibition of cells with the MET wild-type sequence[1].
    Merestinib (2, 5, and 10 μM) reduces the number of viable TFK-1 and SZ-1 cells in a dose and time dependent manner, and significant inhibits wound healing for TFK-1 and SZ-1 cell lines. Merestinib inhibits cell invasion in TFK-1 and SZ-1 cells in a concentration dependent manner[2].

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

    Merestinib dihydrochloride 相关抗体:
    体内研究
    (In Vivo)

    Merestinib (LY2801653) demonstrates anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87MG, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects. Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a pharmacodynamic residence time (Koff) of 0.00132 min-1 and t1/2 of 525 min. Merestinib (LY2801653) treatment inhibits MET phosphorylation with a composite TED50 (50 % target inhibition dose) of 1.2 mg/kg and a composite TED90 (90 % target inhibition dose) of 7.4 mg/kg[1]. Merestinib (LY2801653) (20 mg/kg) reduces TFK-1 tumor growth significantly relative to vehicle control. Merestinib (LY2801653) inhibits the growth of intra- and extrahepatic CCC xenograft tumors[2].

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

    625.45

    Formula

    C30H24Cl2F2N6O3
    CAS 号
    性状

    固体

    颜色

    White to light yellow

    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
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (159.88 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.5988 mL 7.9942 mL 15.9885 mL
    5 mM 0.3198 mL 1.5988 mL 3.1977 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

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.00 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.00 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

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

    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.36%

    COA (272 KB) LCMS (97 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    The Ki value and mode of inhibition of LY2801653 for the MET kinase activity are determined using a radiometric filter-binding assay. Reactions are carried out in 96-well plates in Enzyme dilution buffer (EDB) compose of 50 mM Tris HCl pH 7.5, 2 mM DTT, 0.005% Triton X-100, 10 mM MgCl2, and 250 μM EDTA. Serially diluted LY2801653 (final concentration 250 to 0 nM) are followed by the addition of a series of 8 concentrations of 33P-γ-ATP (final concentration 400 to 10 μM ATP), and 5 nM enzyme (final concentration). After a 2-hour incubation, PolyGluTyr synthetic protein substrate (final 150 μg/mL) is added to initiate the 30-minute kinase reaction. Reactions are quenched with 10% H3PO4, transfer to a pre-wetted Multiscreen anionic phosphocellulose 96-well filter plate, and washed; radioactivity is measured with a scintillation counter. The experimental data are fit to a global mix model inhibition equation using GraphPad Prism softwar to generate an alpha value to determine the modality of inhibition and to calculate the Ki value for LY2801653[1].

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

    H460 cells are cultured in RPMI media supplemented with 10% FBS and plated (prior to becoming 70% confluent) in 96-well plates at 20,000 cells/well and are incubated overnight at 37°C. The next day, the cells are incubated with RPMI-1640 in low serum (0.5% FBS) for 2 hours prior to treatment with Merestinib. Thirty minutes after the addition of Merestinib (LY2801653), HGF at a final concentration of 100ng/mL is added. After a 10-minute incubation, cell lysates are prepared and pMET is quantified. Relative IC50 values are determined using MSD activity units by calculating the percentage of inhibition with respect to on-plate MIN (unstimulated) and MAX controls and then fitting the percentage-of-inhibition values and 10-point dose response data to a 4-parameter logistic equation using ActivityBase[1].

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

    S114 cells are implanted subcutaneously onto female athymic nude mice. For dose response evaluation, on day 8 after the implantation, Merestinib (LY2801653) is given at a range of 0.75 mg/kg to 100 mg/kg (n=8 per dose group). At 2 hours after dose, blood samples and tumors are collected and flash frozen. For time course study, Merestinib (LY2801653) is given at 12 mg/kg (n=10 per time point). Animals are sacrificed at 2, 8, 16, and 24 hours after dose, and blood samples and tumors are collected. pMET is measured in the S114 tumor lysates using the MSD ELISA assay. Lysates are prepared from pulverized frozen tumor tissue, and homogenized with Lysing Matrix D beads, with addition of RIPA lysis buffer containing phosphatase and protease inhibitors. Protein concentration is determined using the DC protein assay kit. The pMET MSD ELISA assay is performed.

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

    Merestinib dihydrochloride 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 1.5988 mL 7.9942 mL 15.9885 mL 39.9712 mL
    5 mM 0.3198 mL 1.5988 mL 3.1977 mL 7.9942 mL
    10 mM 0.1599 mL 0.7994 mL 1.5988 mL 3.9971 mL
    15 mM 0.1066 mL 0.5329 mL 1.0659 mL 2.6647 mL
    20 mM 0.0799 mL 0.3997 mL 0.7994 mL 1.9986 mL
    25 mM 0.0640 mL 0.3198 mL 0.6395 mL 1.5988 mL
    30 mM 0.0533 mL 0.2665 mL 0.5329 mL 1.3324 mL
    40 mM 0.0400 mL 0.1999 mL 0.3997 mL 0.9993 mL
    50 mM 0.0320 mL 0.1599 mL 0.3198 mL 0.7994 mL
    60 mM 0.0266 mL 0.1332 mL 0.2665 mL 0.6662 mL
    80 mM 0.0200 mL 0.0999 mL 0.1999 mL 0.4996 mL
    100 mM 0.0160 mL 0.0799 mL 0.1599 mL 0.3997 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:

    Merestinib1206801-37-7LY2801653LY 2801653LY-2801653c-Met/HGFRFLT3ROS KinaseDiscoidin Domain ReceptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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