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  2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Met/HGFR Apoptosis
  4. Capmatinib

Capmatinib  (Synonyms: 卡馬替尼; INC280; INCB28060)

目錄號: HY-13404 純度: 99.92%
COA 產(chǎn)品使用指南

Capmatinib (INC280; INCB28060) 是一種有效的、口服活性的、選擇性的、ATP 競爭性的 c-Met 激酶抑制劑 (IC50=0.13 nM)。Capmatinib 可抑制 c-MET 的磷酸化，以及 c-MET 通路下游效應蛋白如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。Capmatinib 有效抑制 c-Met 依賴性腫瘤細胞的增殖和遷移，并有效誘導細胞凋亡。在腫瘤小鼠模型中表現(xiàn)出抗腫瘤活性。Capmatinib 主要由 CYP3A4 和醛氧化酶代謝。

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Capmatinib Chemical Structure

Capmatinib Chemical Structure

CAS No. : 1029712-80-8

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥869
In-stock
1 mg ￥320
In-stock
5 mg ￥790
In-stock
10 mg ￥950
In-stock
25 mg ￥1950
In-stock
50 mg ￥3100
In-stock
100 mg ￥4850
In-stock
200 mg 現(xiàn)貨 詢價
500 mg   詢價  
1 g   詢價  

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Customer Review

    Capmatinib purchased from MCE. Usage Cited in: Department Cancer Biology. Wayne State University. 2014 Jan.

    The c-Met Inhibitor INC280 Reveals HGF Activation of c-Met Leads to β4 Activation. (A) Dose-dependent assay to determine the concentration of INC280 required to prevent HGF-induced c-Met phosphorylation. Cells are pre-treated for two hours with INC280 at the indicated concentrations and then stimulated with 50 ng/mL HGF for 30 minutes. Phosphorylated (upper panel) and total c-Met (lower panel) are analyzed by Western blot. Densitometry represents the ratio of phosphorylated to total c-Met as a p

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].

    IC50 & Target

    IC50: 0.13 nM (c-MET)[1]
    體外研究
    (In Vitro)

    Capmatinib (INCB28060) 抑制 c-MET 磷酸化，IC50 值約為 1 nM，濃度約為 4 nM 時抑制 c-MET 超過 90%，這是可逆的，在去除化合物后的數(shù)小時內(nèi)效果顯著降低，48 小時后完全消失[1]。
    Capmatinib (INCB28060) (0-10000 nM；72 小時) 抑制 SNU-5，S114、H441 和 U-87MG 的增殖[1]。
    Capmatinib (INCB28060) (0.06-62.25 nM；2h) 有效抑制 c-MET 磷酸化以及 c-MET 通路下游效應子，例如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5[1]。
    Capmatinib (INCB28060) (0.24-63 nM；過夜) 可防止 HGF 刺激的 H441 細胞遷移[1]。
    Capmatinib (INCB28060) (0.5-50 nM；20 分鐘) 可快速抑制 EGFR 和 HER-3 的磷酸化[1]。
    Capmatinib (INCB28060) (0-333 nM；24 h) 誘導 SNU-5 細胞凋亡[1]。

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

    Cell Viability Assay[1]

    Cell Line: SNU-5, S114, H441 and U-87MG
    Concentration: 0-10000 nM
    Incubation Time: 72 h
    Result: Inhibited the cell viability of SNU-5 and S114, as well as the colony formation of H441 and U-87MG, with IC50 values of 1.2 nM, 12.4 nM, ~0.5 nM and 2 nM, respectively.

    Cell Migration Assay [1]

    Cell Line: H441 (stimulated with 50 ng/mL recombinant human HGF for 24h)
    Concentration: 0.24, 1, 4, 16 and 63 nM
    Incubation Time: Over night
    Result: Prevented HGF-stimulated H441 cell migration, with IC50 of approximately 2 nM, and less cell migration at 16 nM.

    Western Blot Analysis[1]

    Cell Line: SNU-5
    Concentration: 0.06, 0.24, 0.98, 3.91, 15.63 and 62.25 nM
    Incubation Time: 2 h
    Result: Effectively inhibited phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5.

    Western Blot Analysis[1]

    Cell Line: H1993 cells
    Concentration: 0.5, 5 and 50 nM
    Incubation Time: 20 min
    Result: Suppressed phosphorylation of both EGFR and HER-3 rapidly and as effectively as the compound inhibited c-MET phosphorylation in H1993 cells.

    Apoptosis Analysis[1]

    Cell Line: SNU-5 cells
    Concentration: 0.017, 0.15, 1.37, 12.33, 111 and 333 nM
    Incubation Time: 24 h
    Result: Effectively induced DNA fragmentation.
    體內(nèi)研究
    (In Vivo)

    Capmatinib (INCB28060) (1-30 mg/kg；PO，每天兩次，持續(xù) 2 周) 對腫瘤生長具有劑量依賴性抑制作用，并且在處理期間對所有劑量均表現(xiàn)出良好的耐受性，沒有明顯的毒性或體重的的損失證據(jù)在 U-87MG 腫瘤小鼠模型[1]。
    Capmatinib (INCB28060) (0.03-10 mg/kg；PO，單劑量) 抑制 S114 腫瘤中的 c-MET 磷酸化小鼠模型[1]。

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

    Animal Model: Female Balb/c nu/nu mice (inoculated subcutaneously with 5×106 U-87MG glioblastoma cells)[1]
    Dosage: 1, 3, 10 and 30 mg/kg
    Administration: PO, twice daily, for 2 weeks
    Result: Exhibited dose-dependent inhibition of tumor growth with 35% and 76% at 1 and 3 mg/kg once daily; resulted in partial regressions in 6 of 10 U-87MG tumor-bearing mice at 10 mg/kg once daily; and showed well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss.
    Animal Model: Female Balb/c nu/nu mice (inoculated subcutaneously with 4×106 S114 tumor cells)[1]
    Dosage: 0.03, 0.1, 0.3, 1, 3 and 10 mg/kg
    Administration: PO, single dosage
    Result: Caused approximately 50% and 90% inhibition of c-MET phosphorylation at 0.03 and 0.3 mg/kg after administration of 30 min, and inhibition of phospho-c-MET exceeded 90% after 7 hours.
    Clinical Trial
    分子量

    412.42

    Formula

    C23H17FN6O
    CAS 號
    性狀

    固體

    顏色

    Light yellow to yellow

    中文名稱

    卡馬替尼；苯扎米特
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 5 mg/mL (12.12 mM; 超聲助溶 (<60°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 : < 0.1 mg/mL (insoluble)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.4247 mL 12.1236 mL 24.2471 mL
    5 mM 0.4849 mL 2.4247 mL 4.8494 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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)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： 0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (24.25 mM); 懸濁液; 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: 99.92%

    參考文獻

    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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4247 mL 12.1236 mL 24.2471 mL 60.6178 mL
    5 mM 0.4849 mL 2.4247 mL 4.8494 mL 12.1236 mL
    10 mM 0.2425 mL 1.2124 mL 2.4247 mL 6.0618 mL
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      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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