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。

ARQ 531

CAS No. : 2095393-15-8

MCE 国际站：ARQ 531

产品活性：ARQ 531 (MK-1026) 是 BTK 可逆的、非共价的、具有口服活性的抑制剂，其对 WT-BTK 和 C481S-BTK 的 IC₅₀ 值分别为 0.85 nM 和 0.39 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: ARQ 531 shows strong target inhibition in TMD8 cell line. The IC₅₀ values are 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively, in biochemical assay. Additionally, ARQ 531 also shows strong inhibition of TEK kinases with IC₅₀s of 5.23 nM (BMX), 5.80 nM (TEC), 36.4 nM (TXK). The IC₅₀s of ARQ 531 for SRC kinases are 3.86 nM (LCK), 4.22 nM (YES), 9.71 nM (BLK), 18.3 nM (HCK), 18.8 nM (LYNa), 25.9 nM (FGR), 32.2 nM (FYN), 48.0 nM (FRK) and for TRK kinases are 11.7 nM (TrkB), 13.1 nM (TrkA), 19.1 nM (TrkC). ARQ 531 inhibits proliferation of diverse types of cell lines (TMD8: GI₅₀=0.13 μM, REC1: GI₅₀=0.18 nM) and shows potency in cell lines that are addict to BCR, Src-family kinase and PI3K/AKT pathways.

In Vivo: ARQ 531 is efficacious in TMD-8 tumor xenograft model. ARQ 531 causes complete tumor regression after 14 days of treatment. ARQ 531 is also efficacious in collagen induced arthritis model. ARQ 531 demonstrates potent efficacy against arthritis in mouse model. In the BTK driven TMD8 xenograft mouse model, ARQ 531 demonstrates excellent anti-tumor activity with durable response. ARQ 531 demonstrates in vivo efficacy in a mouse collagen-induced arthritis (CIA) model.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Atuzabrutinib  |  PCI 29732  |  JAK3/BTK-IN-6  |  Pirtobrutinib  |  CNX-500  |  BTK inhibitor 17  |  Remibrutinib  |  RN486  |  GDC-0834 Racemate  |  Spebrutinib besylate  |  BTK inhibitor 19  |  BMX-IN-1  |  BMS-935177  |  Ibrutinib  |  PF-06250112  |  QL-X-138  |  SJF620 hydrochloride  |  PROTAC BTK Degrader-2  |  BTK-IN-8  |  JAK3/BTK-IN-3  |  JS25  |  JAK3/BTK-IN-2  |  (R)-Zanubrutinib  |  Edralbrutinib  |  Branebrutinib  |  Poseltinib  |  BTK inhibitor 20  |  RET-IN-14  |  QL47  |  BTK-IN-23

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

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；
•   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。