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

Merestinib (Synonyms: LY2801653)

製品番号: HY-15514 純度: 99.99%
取扱説明書

Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) 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).

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Merestinib 構造式

Merestinib 構造式

CAS 番号 : 1206799-15-6

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 160 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 132 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 180 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 540 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 768 在庫あり
Estimated Time of Arrival: December 31
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500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Merestinib:

Top Publications Citing Use of Products

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

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

    Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) 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]

    体外実験

    Merestinib (LY2801653) demonstrates effects on MET pathway-dependent cell scattering and cell proliferation. The mean IC50 value (n=6 determinations) of Merestinib (LY2801653) 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. 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].
    Transfection with the MET variants confers growth-factor independence and treatment with Merestinib (LY2801653) 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 (LY2801653) (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 (LY2801653) inhibits cell invasion in TFK-1 and SZ-1 cells in a concentration dependent manner[2].

    体内実験

    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].

    臨床実験
    分子量

    552.53

    分子式

    C₃₀H₂₂F₂N₆O₃

    CAS 番号

    1206799-15-6

    SMILES

    O=C(C1=CC=C(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=CC5=C(N(C)N=C5)C=C4C6=CNN=C6)C(F)=C3

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 32 mg/mL (57.92 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8099 mL 9.0493 mL 18.0986 mL
    5 mM 0.3620 mL 1.8099 mL 3.6197 mL
    10 mM 0.1810 mL 0.9049 mL 1.8099 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [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 (LY2801653). 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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [1]

    Mice[1]
    S114 cells are implanted subcutaneously onto female athymic nude mice. For dose response evaluation, on day 8 after the implantation, Merestinib 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 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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献
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    Keywords:

    MerestinibLY2801653LY 2801653LY-2801653c-Met/HGFRFLT3ROSDiscoidin Domain ReceptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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    製品名:
    Merestinib
    製品番号:
    HY-15514
    数量:
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