2. Protein Tyrosine Kinase/RTK Autophagy
  3. c-Met/HGFR Autophagy
  4. Tepotinib hydrochloride

Tepotinib hydrochloride  (Synonyms: EMD-1214063 hydrochloride)

目录号: HY-14721A
产品使用指南

摩尔计算器

Tepotinib (EMD-1214063) hydrochloride 是一种具有口服活性的、高度选择性，可逆的，ATP-竞争性的 c-Met 抑制剂，IC50 为 3 nM，对 c-Met 的选择性比 IRAK4，TrkA，Axl，IRAK1 和 Mer 高 200 倍以上。Tepotinib hydrochloride 抑制 c-Met 磷酸化，诱导自噬 (autophagy)。Tepotinib hydrochloride 具有抗肿瘤作用。

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Tepotinib hydrochloride Chemical Structure

Tepotinib hydrochloride Chemical Structure

CAS No. : 1103508-80-0

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Tepotinib hydrochloride 的其他形式现货产品:

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Tepotinib hydrochloride 相关抗体

Top Publications Citing Use of Products

    Tepotinib hydrochloride purchased from MCE. Usage Cited in: Gene Expr. 2018 May 18;18(2):135-147.  [Abstract]

    Western blot for Myc-tag shows decrease in Myc-tag levels at 8 weeks of EMD1214063 treatment only. GAPDH shows comparable loading in all lanes.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects[1][2][3].

    体外研究
    (In Vitro)

    Tepotinib hydrochloride 抑制 IRAK4、TrkA、Axl、IRAK1、Mer 和 TrkA，IC50 分别为 615、1017、1566、2037、2272 和 5716 nM[1]。
    Tepotinib hydrochloride 抑制 A549 细胞中     HGF 诱导的 c-Met 磷酸化，平均 IC50 为 6 nM[1]。
    Tepotinib (0.01 nM-30 μM) hydrochloride 可在体外抑制肿瘤细胞增殖和迁移[1]。

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

    Tepotinib hydrochloride 相关抗体:
    体内研究
    (In Vivo)

    Tepotinib hydrochloride 在异种移植模型中诱导肿瘤消退并抑制体内 c-Met 磷酸化[1]。

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

    Animal Model: CD-1 or BALB/C nude mice bearing human cancer cell lines KP-4, or EBC-1[1]
    Dosage: 6 and 15 mg/kg for mice bearing NSCLC EBC-1; 25, 50 and 200 mg/kg for mice bearing pancreatic carcinoma cell line KP-4.
    Administration: Injected daily; for 14-18 days
    Result: Daily administration of 5 or 15 mg/kg to EBC-1 tumor-bearing mice resulted in effective inhibition or complete tumor regression, respectively.
    Induced dose-dependent tumor growth inhibition in mice bearing human pancreatic carcinoma KP-4 tumors.
    分子量

    492.57 (free base)

    Formula

    C29H28N6O2.xHCl
    CAS 号
    运输条件

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

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Tepotinib hydrochloride 相关分类

    • 摩尔计算器

    • 稀释计算器

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    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:

    Tepotinib1103508-80-0EMD-1214063EMD1214063EMD 1214063c-Met/HGFRAutophagyantitumorHs746Tgastric cancerNSCLCInhibitorinhibitorinhibit

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