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。
PHA-665752
CAS No. : 477575-56-7
MCE 国际站：PHA-665752
产品活性：PHA-665752 是一种选择性的 ATP 竞争活性位点 c-Met 激酶抑制剂，Ki 为 4 nM，IC50为 9 nM。PHA-665752 对 c-Met 的选择性比一组不同的酪氨酸和丝氨酸苏氨酸激酶高 50 倍。PHA-665752 诱导细胞凋亡和细胞周期阻滞，具有细胞还原性抗肿瘤活性。
研究领域：Protein Tyrosine Kinase/RTK | Autophagy | Apoptosis
作用靶点：c-Met/HGFR | Autophagy | Apoptosis
In Vitro: PHA-665752 is a potent and ATP-competitive inhibitor of c-Met kinase activity with a Ki of 4 nM and an IC50 of 9 nM.
PHA-665752 exhibits >50-fold selectivity for c-Met enzyme compared with the majority of kinases evaluated.
PHA-665752 shows potent inhibition of c-Met RTK autophosphorylation in NIH3T3 cells engineered to express high levels of c-Met and hepatocyte growth factor (HGF).
PHA-665752 inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines.
PHA-665752 (0-1.25 μM; 18 hours) potently inhibits HGF and c-Met-driven phenotypes such as cell growth (proliferation and survival), cell motility, invasion, and/or morphology of a variety of tumor cells.
PHA-665752 (0-1.25 μM; 72 hours) induces apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells.
PHA-665752 (0.0125-0.2 μM; 4 hours) potent inhibits HGF-induced c-Met phosphorylation in A549 cells.
In Vivo: PHA-665752 (7.5-30 mg/kg/day; i.v. ; for 9 days) exhibits statistically significant dose-dependent tumor growth inhibition of 68%, 39%, and 20% of vehicle control at the 30 mg/kg/day, 15 mg/kg/day, and 7.5 mg/kg/day doses, respectively.
PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model.
相关产品：Bioactive Compound Library Plus | Apoptosis Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Lung Cancer Compound Library | Angiogenesis-Related Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | Cytokine Inhibitors Library | Cell Death Library | Anti-Ovarian Cancer Compound Library | Bioactive Compound Library Max | Anti-Gastric Cancer Compound Library | MG-132 | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Y-27632 | Paclitaxel | Z-VAD-FMK | LY294002 | 2-Deoxy-D-glucose | Angiotensin II human | Acetylcysteine | Staurosporine | Actinomycin D | SB-431542 | 5-Fluorouracil | Bortezomib | Oxaliplatin | Deferoxamine mesylate | Sorafenib | Trametinib | Gemcitabine | Temozolomide | Etoposide | Rotenone | Mdivi-1 | Monomethyl auristatin E | Decitabine | Ruxolitinib | Elesclomol | DAPT
热门产品线：重组蛋白 | 药物筛选 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
• 50,000 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；
• 产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
• 提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
• 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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
• 专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
• 与世界各大制药公司及知名科研机构建立了长期的合作。
