NVP-TAE 226 | MedChemExpress (MCE)

NVP-TAE 226 产品活性：NVP-TAE 226 (TAE226) 是一种有效且具有 ATP 竞争性的双重 FAK 和 IGF-1R 抑制剂，IC50 分别为 5.5 nM、140 nM。NVP-TAE 226 (TAE226) 还有效抑制 Pyk2，胰岛素受体 (InsR)，IC50 分为 3.5 nM、40 nM。 产品来源： https://www.medchemexpress.cn/NVP-TAE-226.html 研究领域：Protein Tyrosine Kinase/RTK | Apoptosis 作用靶点：FAK | Pyk2 | IGF-1R | Insulin Receptor | Apoptosis In Vitro: NVP-TAE 226 (TAE226), a potent ATP-competitive inhibitor of several tyrosine protein kinases, in particular FAK and IGF-IR kinases. In a cell-based kinase assays, FAK, IGF-IR kinase, and IR kinase are inhibited with an IC50 range of 100 to 300 nM compared with the other kinases tested, which are >10-fold less sensitive. In culture, NVP-TAE 226 inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr395). NVP-TAE 226 also inhibits IGF-I-induced phosphorylation of IGF-IR and activity of its downstream target genes such as MAPK and Akt. NVP-TAE 226 retards tumor cell growth as assessed by a cell viability assay and attenuates G2-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr15) protein expression. NVP-TAE 226 treatment inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay. Interestingly, TAE226 treatment of tumor cells containing wild-type p53 mainly exhibits G2-M arrest, whereas tumor cells bearing mutant p53 underwent apoptosis. In Vivo: Treatment with NVP-TAE 226 (TAE226) at 50 or 75 mg/kg extends the median survival of U87 xenograft animals by 6 and 7 days, respectively (P=0.084 and P=0.042, respectively, compared with vehicle-treated animals). However, NVP-TAE 226 treatment of LN229-engrafted animals significantly prolongs their median survival by 19 days (P<0.004 for both dosages, compared with vehicle-treated animals). 相关产品：Bioactive Compound Library Plus | Apoptosis Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Endocrinology Compound Library | Cytoskeleton Compound Library | Anti-Pancreatic Cancer Compound Library | Angiogenesis-Related Compound Library | Human Metabolite Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Metabolic Enzyme Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Cytokine Inhibitors Library | Cell Death Library | Multi-Target Compound Library | Radiosensitizer Library | Bioactive Compound Library Max | MG-132 | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Y-27632 | LY294002 | Paclitaxel | Z-VAD-FMK | Acetylcysteine | Angiotensin II human | 2-Deoxy-D-glucose | Staurosporine | Actinomycin D | SB-431542 | 5-Fluorouracil | Bortezomib | Deferoxamine mesylate | Oxaliplatin | Trametinib | Sorafenib | Temozolomide | Gemcitabine | Decitabine | Mdivi-1 | Rotenone | Etoposide | Elesclomol | Insulin (human) | Ruxolitinib | Monomethyl auristatin E 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最新最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。

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