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. : 1551355-46-4
MCE 国际站:Simmiparib
产品活性:Simmiparib 是一种高效且具有口服活性的 PARP1 和 PARP2 抑制剂,IC50 分别为 1.75 nM 和 0.22 nM。Simmiparib 对 PARP1/2 的抑制作用强于其母体化合物 Olaparib (HY-10162)。在同源重组修复 (HR) 缺陷细胞中,Simmiparib 诱导 DNA 双链断裂 (DSB) 积累和 G2/M 阻滞,从而诱导细胞凋亡 (apoptosis)。Simmiparib 在细胞和裸鼠移植瘤模型中都表现出显著的抗癌活性。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:PARP
In Vitro: Simmiparib (0-10 μM; 3 days) exhibits anti-proliferative activity against various cancer cells.
Simmiparib (0-10 μM; 48 h) induces typical G2/M arrest in Capan-1 cells.
Simmiparib (0.1-2 μM; 24 h) induces apoptosis in MDA-MB-436 and V-C8 (BRCA2-/-) cells, and increases dose-dependently the levels of γH2AX.
Simmiparib (1-10 μM; 48 h or 72 h) increases the phosphorylation levels of Chk1 and Chk2 and the protein levels of p-Cyclin B1 (S147), Cyclin B1, p-CDK1 (Y15) and CDK1.
In Vivo: Simmiparib (2, 4 and 8 mg/kg; p.o.; qd, for 14 days) inhibits the growth of tumor in V-C8 (BRCA2-/-) and MDA-MB-436 (BRCA2-/-) xenograft mice models.
Simmiparib (10 and 50 mg/kg; p.o.; qd, for 42 days) inhibits the growth of BRCA1-mutated breast cancer in xenograft mice model.
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 | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | iRucaparib-AP6 | Rucaparib monocamsylate | AZD-2461 | 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
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。