卡马替尼 T1963

Product Introduction
Bioactivity


英文名: Capmatinib

描述: Capmatinib (INCB28060) 是一种具有口服活性的，选择性的，ATP 竞争性的c-Met 激酶抑制剂，IC50值为0.13 nM。它有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移，可诱导细胞凋亡，有抗肿瘤活性。

细胞实验: H441 cells are seeded in RPMI-1640 medium containing 10% FBS and grown to complete confluence. Gaps are introduced by scraping cells with a P200 pipette tip. Cells are then stimulated with 50 ng/mL recombinant human HGF to induce migration across the gap in the presence of various concentrations of INCB28060. After an overnight incubation, representative photographs are taken and a semiqualitative assessment of inhibition of cell migration is conducted.(Only for Reference)

激酶实验: c-Met Kinase Assay: The assay buffer contains 50 mM Tris-HCl, 10 mM MgCl2, 100 mM NaCl, 0.1 mg/ml BSA, 5 mM DTT, pH 7.8. For HTS 0.8 μL of 5 mM of INCB28060 dissolved in DMSO are dotted on 384-well plates. DMSO titration suggests that the maximum tolerated concentration of the solvent is 4%. To measure IC50s the INCB28060 plate is prepared by 3-fold and 11-point serial dilutions. 0.8 μL of INCB28060 in DMSO is transferred from INCB28060 plate to the assay plate. The final concentration of DMSO is 2%. Solutions of 8 nM unphosphorylated c-Met or 0.5 nM phosphorylated c-Met are prepared in assay buffer. A 1 mM stock solution of peptide substrate Biotin-EQEDEPEGDYFEWLE-amide dissolved in DMSO is diluted to 1 μM in assay buffer containing 400 μM ATP (unphosphorylated c-Met) or 160 uM ATP (phosphorylated c-Met). A 20 μL volume of enzyme solution (or assay buffer for the enzyme blank) is added to the appropriate wells in each plate and then 20 μL/well of substrate solution to initiate the reaction. The plate is protected from light and incubated at 25 °C for 90 minutes. The reaction is stopped by adding 20 μL of a solution containing 45 mM EDTA, 50 mM Tris-HCl, 50 mM NaCl, 0.4 mg/ml BSA, 200 nM SA-APC and 3 nM EUPy20. The plate is incubated for 15-30 minutes at room temperature and HTRF (homogenous time resolved fluorescence) is measured on a Perkin Elmer Fusion α-FP instrument. The HTRF program settings used are as follows: Primary excitation filter 330/30, Primary window: 200 uSec, Primary delay: 50 uSec, Number of flashes: 15, Well read time: 2000

体外活性: 在c-MET依赖的小鼠肿瘤模型中,口服INCB28060（0.03 mg/kg）能够有效抑制肿瘤生长.

体内活性: 在肿瘤细胞中,INCB28060通过下调c-MET磷酸化以及c-MET介导的信号转导,抑制细胞增殖和存活。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.12 mg/mL (10 mM)


关键字: orally active | Capmatinib | Apoptosis | ATP competitive | H441 | Balb/c nu/nu mice | NVP-INC-280 | inhibit | INC 280 | c-Met/HGFR | Inhibitor | INC280 | SNU-5 | INCB 28060 | NVP-INC 280 | U-87MG | INCB-28060 | S114

相关产品: Citric acid | Mezigdomide | Taurochenodeoxycholic Acid | AGN 192870 | Terfenadine | NSC 23766 trihydrochloride | PND-1186 | Tauroursodeoxycholate sodium | ZINC69391 | ZM-447439

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途