FGFR-IN-13 产品活性:FGFR-IN-13 (compound III-30) 通过抑制关键蛋白的表达调节内源性 FGFR1(IC50=0.20±0.02 nM) 和 FGFR4(IC50=0.40±0.03 nM) 介导的信号通路。FGFR-IN-13 能够抑制 total-PARP 和 Bcl-2 蛋白的表达,促进 Cleaved-PARP 和 Bax 蛋白的表达,且呈剂量依赖性。FGFR-IN-13 具有显著的抗肿瘤活性且具有口服活性。 产品来源: www.medchemexpress.cn/fgfr-in-13.html 研究领域:Protein Tyrosine Kinase/RTK 作用靶点:FGFR In Vitro: FGFR-IN-13 (10 μM, 9 h) can achieve covalent irreversibly binding with FGFR protein. FGFR-IN-13 inhibits p-FGFR protein expression can reach the level of AZD4547 (HY-13330) and TAS-120 (HY-100818) in MDA-MB-231 cells. FGFR-IN-13 (2.5, 5, 10 μM, 24 h) has better apoptosis-inducing ability than AZD4547 (45.4 % versus 37.3 %) at the same concentration (5 μM) and has a similar mechanism of action to AZD4547, but MDAMB-231 cells are much sensitive to III-30. FGFR-IN-13 (1.25, 2.5, 5 μM, 12 h) inhibits the migration of triple-negative breast cancer cells compatible to AZD4547 at the same concentration. FGFR-IN-13 (2.5, 5, 10 μM, 12 h) is capable of inducing cell apoptosis by generating excess ROS and decreasing MMP. In Vivo: FGFR-IN-13 (10 and 30 mg/kg, po; everyday for 21 days) inhibits tumor growth in a dose-dependent manne. FGFR-IN-13 has a favorable safety profile and is effective in inhibiting tumor growth at safe doses in MDA-MB-231 xenograft tumor mouse mode. 相关产品:Lenvatinib | Regorafenib | Nintedanib | Ponatinib | Erdafitinib | Infigratinib | Pemigatinib | Heparan Sulfate | Pazopanib | Futibatinib | Formononetin | Fexagratinib | PD173074 | SU 5402 | Masitinib | Dovitinib | Ferulic acid | KW-2449 | Triamcinolone acetonide | PD-166866 | Fisogatinib | BLU9931 | Gandotinib | Sulfatinib | Lirafugratinib | Roblitinib | LY2874455 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前沿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TOP期刊及制药专利收录了MCE客户的科研成果;专业团队跟踪前沿的制药及生命科学研究进展,为您提供全球前沿的活性化合物;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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