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Capmatinib 2HCl

Capmatinib 2HCl

产品编号 T4260   CAS 1197376-85-4
别名: INC-280 2HCl, INCB28060盐酸盐, INCB28060 2HCl

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

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Capmatinib 2HCl Chemical Structure
Capmatinib 2HCl, CAS 1197376-85-4
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
其他形式的 Capmatinib 2HCl:
产品目录号及名称: Capmatinib 2HCl (T4260)
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生物活性
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存储 & 溶解度
参考文献
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

存储

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

溶解度

DMSO: 11 mg/mL (22.66 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Liu X, et al,A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res, 2011, 17(227). 7127-7138.
JNJ-38877618 SU11274 SGX-523 c-Met-IN-17 Terevalefim Herbacetin Foretinib Cabozantinib S-malate

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 酪氨酸激酶分子库 抗癌上市药物库 抗癌药物库 表型筛选靶点鉴定库 抑制剂库 经典已知活性库 FDA上市及药典收录分子库 已知活性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
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每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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技术支持

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。

Keywords

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

 

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