Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Capmatinib 2HCl (INC-280 2HCl) 是一种新型的 ATP 竞争性 c-MET 激酶抑制剂,IC50 为 0.13 nM。它具有皮摩尔酶效,对 c-MET 具有高度特异性,选择性超过 10, 000 倍一大组人类激酶。该抑制剂在 c-MET 依赖性肿瘤细胞系中有效阻断 c-MET 磷酸化和其关键下游效应子的激活。因此,它在体外有效抑制 c-MET 依赖性肿瘤细胞增殖和迁移,并有效诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 226 | 现货 | ||
2 mg | ¥ 313 | 现货 | ||
5 mg | ¥ 632 | 现货 | ||
10 mg | ¥ 770 | 现货 | ||
25 mg | ¥ 1,460 | 现货 | ||
50 mg | ¥ 2,630 | 现货 | ||
100 mg | ¥ 3,920 | 现货 | ||
500 mg | ¥ 8,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 697 | 现货 |
产品描述 | Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10, 000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro. |
靶点活性 | c-Met (cell-free assay):0.13 nM |
体外活性 | INCB28060(free base)exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10,000-fold selectivity over a large panel of human kinases. INCB28060 inhibits human c-MET phosphorylation and c-MET-mediated signaling in cancer cells. INCB28060 inhibits c-MET-dependent cell proliferation and survival, and prevents anchorage-independent cancer cell growth and cell migration. |
体内活性 | INCB28060(free base) shows strong antitumor activity in c-MET-dependent mouse tumor models, even oral treatment of 0.03 mg/kg INCB28060 causes approximately 50% inhibition of c-MET-phosphorylation. Dose-dependent inhibition of tumor growth is observed in tumor-bearing mice. |
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 |
细胞实验 | Cell lines: H441 cells. Concentrations: 0.24,1,4,16,63 nM. Incubation Time: 24 hours. Method: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. |
动物实验 | Animal Models: Eight-week-old female Balb/c nu/nu mice (Charles River) are inoculated subcutaneously with 4 × 106 tumor cells (S114 model) or with 5 × 106 tumor cells (U-87 mg glioblastoma model). Formulation: INCB28060 is prepared as a 5 mM stock solution in 100% dimethyl sulfoxide and routinely stored at room temperature. Dosages: 3,10,30 mg/kg. Administration: INCB28060 is orally dosed,twice each day. |
别名 | INC-280 2HCl, INCB28060盐酸盐, INCB28060 2HCl |
分子量 | 485.34 |
分子式 | C23H19Cl2FN6O |
CAS No. | 1197376-85-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11 mg/mL (22.66 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0604 mL | 10.3021 mL | 20.6041 mL | 51.5103 mL |
5 mM | 0.4121 mL | 2.0604 mL | 4.1208 mL | 10.3021 mL | |
10 mM | 0.206 mL | 1.0302 mL | 2.0604 mL | 5.151 mL | |
20 mM | 0.103 mL | 0.5151 mL | 1.0302 mL | 2.5755 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Capmatinib 2HCl 1197376-85-4 Tyrosine Kinase/Adaptors c-Met/HGFR Apoptosis H441 orally active SNU-5 INCB28060 Inhibitor INCB 28060 S114 INC280 INC-280 2HCl inhibit INC 280 Capmatinib INCB-28060 U-87MG ATP competitive INC-280 INCB28060盐酸盐 INCB28060 2HCl Balb/c nu/nu mice inhibitor