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. : 529488-28-6
MCE 国际站:Genz-644282
产品活性:Genz-644282 是一种非喜树碱类拓扑异构酶 I (topoisomerase I) 抑制剂,可用于癌症研究。
研究领域:Cell Cycle/DNA Damage
作用靶点:Topoisomerase
In Vitro: Genz-644282 is a topoisomerase I inhibitor. Genz-644282 shows potent activities against 29 human tumor cell lines with IC50s ranging from 1.8 nM to 1.8 μM. Genz-644282 suppresses the PPTP cell lines, with IC50s of 0.2-21.9 nM, and the mean IC50 value is 1.2 nM. Genz-644282 is potent at trapping Top1-DNA covalent cleavage complexes. Genz-644282 (0.1 μM) induces γH2AX foci in human colon cancer HCT116 cells and breast cancer MCF7 cells. Genz-644282 is cytotoxic on the CPT-resistant human cancer cell lines.
In Vivo: Genz-644282 (1-4 mg/kg) is active when administered intravenously to the mice. Genz-644282 (2.7 mg/kg, i.v.) causes tumor growth delay (TGD) of 34 days in the human HCT-116 colon cancer xenograft, 27 days in the human HT-29 colon carcinoma xenograft and mice bearing the NCI-H460 human non-small cell lung carcinoma. Genz-644282 (2 mg/kg, i.v.) results in a TGD of 33 days in the human HCT-15 colon carcinoma xenograft, and 28 days in mice bearing LOX-IMVI melanoma. Moreover, Genz-644282 (1 mg/kg, i.v.) leads to 14 days of TGD in mice bearing the DLD-1 human colon carcinoma xenograft. Genz-644282 (1.7 mg/kg, i.v.) also produces a TGD of 23 days in mice bearing 786-O tumors and 33 days in NCI-H1299 human non-small cell lung carcinoma xenograft. Genz644282 at maximum tolerated dose (MTD, 4 mg/kg) results in maintained complete responses (MCR) in 6/6 evaluable solid tumor models. Genz644282 (2 mg/kg) induces CR or MCR in 3/3 tumor models and causes objective regressions in 7 of 17 (41%) models, but there are no objective responses at 1 mg/kg.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | Gepotidacin | Topoisomerase IV inhibitor 2 | Phenoxodiol | Topotecan hydrochloride hydrate | NHC-triphosphate tetraammonium | Berberine | Levofloxacin sodium | TAS-103 dihydrochloride | Ciprofloxacin | Mitoxantrone diacetate | Murrayanol | Gimatecan | Camptothecin | EGFR-IN-57 | SW044248 | Topoisomerase I/II inhibitor 4 | NHC-diphosphate triammonium | Betulinic acid | ICRF-196 | 3,6-Diamino-9(10H)-acridone | Epirubicin | 12-Ethyl-9-hydroxycamptothecin | Topoisomerase II inhibitor 3 | Becatecarin | Pixantrone hydrochloride | Datopotamab deruxtecan | Isosteviol
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-16228
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。