Pyrotinib dimaleate | MedChemExpress (MCE)

Pyrotinib dimaleate 产品活性：Pyrotinib dimaleate (SHR-1258 dimaleate) 是有效、选择性的 EGFR/HER2 双重抑制剂，IC 50 值分别为 13 nM 和 38 nM。 产品来源： https://www.medchemexpress.cn/Pyrotinib_dimaleate.html 研究领域：JAK/STAT Signaling | Protein Tyrosine Kinase/RTK 作用靶点：EGFR In Vitro: Pyrotinib dimaleate has high potency in HER2-dependent cell lines (BT474, SK-OV-3), while showing much weaker inhibition in the HER2 negative cell line (MDA-MB-231). Pyrotinib dimaleate inhibits BT474 and SK-OV-3 cells with IC50s of 5.1 and 43 nM, respectively. Pyrotinib dimaleate displays high selectivity as HKI-272 when tested in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and C-Met (c-Src with an IC50 of 790 nM, and others >3000 nM). In Vivo: Pyrotinib dimaleate has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. Pyrotinib dimaleate has favorable drug-like physicochemical properties and shows relatively higher oral exposure in human subjects (oral; t1/2=15 h) with a much longer half life than that of preclinical animal species such as mouse (i.v.; t1/2=1.56 h; i.g.; t1/2=2.52 h) and rat (i.v.; t1/2=4.42 h; i.g.; t1/2=3.38 h). 相关产品：Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | Bioactive Compound Library Plus | Osimertinib | Trastuzumab | Gefitinib | Cetuximab | Erlotinib | Afatinib | Trastuzumab deruxtecan | Lapatinib | AG490 | Genistein | Neratinib | Trastuzumab emtansine | Tucatinib | Dacomitinib | AG-1478 | Pertuzumab | Disitamab vedotin | Mobocertinib | NSC 228155 | Amivantamab | Sapitinib | Pyrotinib | Firmonertinib mesylate | BLU-945 | Patritumab | Lazertinib | Panitumumab 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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