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网站主页 化工产品目录 有机原料 羧酸类化合物及衍生物 卡马替尼盐酸盐 INCB28060盐酸盐
  • INCB28060盐酸盐|T4260|TargetMol

INCB28060盐酸盐|T4260|TargetMol

Capmatinib 2HCl
1197376-85-4
￥226 1mg 起订
￥313 2mg 起订
￥632 5mg 起订
上海 更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
INCB28060盐酸盐
英文名称：
Capmatinib 2HCl
CAS号：
1197376-85-4
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
100%
产品类别：
抑制剂
货号：
T4260

Product Introduction

Bioactivity

名称Capmatinib 2HCl
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.
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.
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
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.
体外活性Capmatinib(free base) 在酶促活性方面表现出皮可摩尔级的效能，并且对于c-MET具有极高的特异性，其选择性比人类大量激酶高出10000倍以上。Capmatinib抑制了人类c-MET的磷酸化和c-MET介导的癌细胞信号传导。此外，Capmatinib阻止了依赖c-MET的细胞增殖和生存，避免了癌细胞在无基底的条件下生长和细胞迁移。
体内活性INCB28060（free base）在依赖c-MET的小鼠肿瘤模型中展现出强大的抗肿瘤活性，即使是0.03 mg/kg的口服剂量也能导致c-MET磷酸化约50%的抑制。在携带肿瘤的小鼠中观察到了剂量依赖性的肿瘤生长抑制。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 11 mg/mL (22.66 mM)
关键字Apoptosis | c-Met/HGFR | H441 | Capmatinib 2HCl | orally active | SNU-5 | INCB28060 | Inhibitor | INCB 28060 | S114 | INC280 | inhibit | INC 280 | Capmatinib | INCB-28060 | U-87MG | ATP competitive | INC-280 | Balb/c nu/nu mice
相关产品Cabozantinib S-malate | Crizotinib | Amuvatinib | BMS 777607 | (±)-Norcantharidin | Capmatinib xHCl | LMTK3-IN-1 | L-Ascorbic acid 2-phosphate trisodium | Norcantharidin | Bacitracin Zinc | AMG-458 | SU11274
相关库抑制剂库 | 抗癌活性化合物库 | 抗癌上市药物库 | 已知活性化合物库 | 激酶抑制剂库 | FDA 上市药物库 | 膜蛋白靶向化合物库 | FDA 上市激酶抑制剂库 | 抗癌临床化合物库 | 抗癌药物库
INCB28060盐酸盐|||INCB28060 2HCl|||INC-280 2HCl|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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