MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Capmatinib dihydrochloride hydrate

CAS No. : 1865733-40-9

MCE 站：Capmatinib dihydrochloride hydrate

产品活性：Capmatinib (INC280; INCB28060) dihydrochloride hydrate 是一种有效的，口服活性的，选择性的，ATP 竞争性的 c-Met 激酶抑制剂 (IC₅₀=0.13 nM)。Capmatinib dihydrochloride hydrate 可抑制 c-MET 的磷酸化，以及 c-MET 通路下游效应蛋白如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。Capmatinib dihydrochloride hydrate 有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移，并有效诱导细胞凋亡。在肿瘤小鼠模型中表现出抗肿瘤活性。Capmatinib dihydrochloride hydrate 主要由 CYP3A4 和醛氧化酶代谢。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：c-Met/HGFR  |  Apoptosis

In Vitro: INCB28060 inhibits c-MET phosphorylation with an IC₅₀ value of approximately 1 nM ａnd a concentration of approximately 4 nM inhibits c-MET more than 90%, which is reversible ａnd the effect is significantly reduced in several hours after the compound is removed ａnd completely disappeared by 48 hours.
INCB28060 (0-10000 nM; 72 h) inhibits the proliferation of SNU-5, S114, H441 ａnd U-87MG.
INCB28060 (0.06-62.25 nM; 2h) effectively inhibits phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, ａnd STAT3/5.
INCB28060 (0.24-63 nM; Over night) prevents HGF-stimulated H441 cell migration.
INCB28060 (0.5-50 nM; 20 min) suppresses phosphorylation of both EGFR ａnd HER-3 rapidly.

In Vivo: INCB28060 (1-30 mg/kg; PO, twice daily, for 2 weeks) exhibits dose-dependent inhibition of tumor growth, ａnd shows well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss in U-87MG tumor mice model.
INCB28060 (0.03-10 mg/kg; PO, single dosage) causes inhibition of c-MET phosphorylation in S114 tumor mice model.

相关产品：MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Y-27632 dihydrochloride  |  Paclitaxel  |  Acetylcysteine  |  Tamoxifen  |  Deferoxamine mesylate  |  Angiotensin II human  |  Staurosporine  |  Bortezomib  |  2-Deoxy-D-glucose  |  5-Fluorouracil  |  Sorafenib  |  SP600125  |  Trametinib  |  Temozolomide  |  Gemcitabine  |  MK-2206 dihydrochloride  |  Decitabine  |  Verteporfin  |  Etoposide  |  Gefitinib  |  Rote  |  DAPT  |  CCCP  |  Ruxolitinib  |  Actinomycin D

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物  |  寡核苷酸

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。