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。
CAS No. : 1174043-16-3
MCE 国际站:AZD-2461
产品活性:AZD-2461 是一种有效的 PARP 抑制剂,可抑制 PARP1,PARP2 和 PARP3 的活性,IC50 值分别为 5 nM,2 nM 和 200 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:PARP
In Vitro: AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively. AZD-2461 (500 nM) shows inhibitory activity against DNA single-strand break repair in human A459 cells. AZD-2461 cuases resistance and high P-gp expression levels in BRCA2-deficient mouse breast cancer line KB2P3.4. AZD-2461 is cytotoxic to BT-20 cells (5-50 μM), increases the proportions of S- and G2-phase BT-20 cells (5-20 μM), and weakly affects the progression of cell cycle in SKBr-3 cells (5-20 μM).
In Vivo: AZD-2461 (10 mg/kg, p.o.) enhances the antitumor activity of temozolomide in a mouse colorectal xenograft and exhibits low effect on mouse bone marrow cells. However, the increased bone marrow tolerability of AZD-2461 is not seen in rat models. AZD-2461 (0.5% v/w HPMC, p.o.) increases the survival of mice bearing KB1P tumors after short-term treatment, and long-term treatment is well tolerated, but can not lead to tumor eradication.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | iRucaparib-AP6 | Rucaparib monocamsylate | RBN-2397 | Rucaparib acetate | Niraparib tosylate | Olaparib-d8 | G007-LK | Basroparib | Anticancer agent 64 | UPF 1069 | Talazoparib tosylate | BPA-B9 | MSC2504877 | Oxychlororaphine | PROTAC PARP1 degrader | 5,7-Dihydroxychromone | PARP1-IN-5 | OUL232 | Stenoparib | PI-1840 | PARP1-IN-11 | 3-Aminobenzamide | PARP1-IN-6 | OM-153 | BRCA1-IN-2 | PARP-2-IN-1 | JQAD1 | Dehydrocorydaline (hydroxyl)
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
货号: HY-13536
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。