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. : 1449746-00-2
MCE 国际站:Mefuparib hydrochloride
产品活性:Mefuparib hydrochloride (MPH) 是一种具有口服活性的,底物竞争性和选择性的 PARP1/2 抑制剂,IC50 分别为 3.2 nM 和 1.9 nM。Mefuparib hydrochloride 诱导细胞凋亡 (apoptosis),并在体内外具有显着的抗癌活性。
研究领域:Cell Cycle/DNA Damage | Epigenetics | Apoptosis
作用靶点:PARP | Apoptosis
In Vitro: Mefuparib hydrochloride (1-10 μM; 48 hours) causes cell apoptosis.
Mefuparib hydrochloride (MPH; 1-10 μM; 24 hours) causes V-C8 cells into typical G2/M arrest.
Mefuparib hydrochloride (1-10 μM; 24 hours) causes the accumulation of DSB marked by the increased levels of γH2AX in the MDA-MB-436 (BRCA1−/−) cells in a concentration-dependent manner.
Mefuparib hydrochloride exerts potent in vitro proliferation-inhibitory effects on cancer cells derived from different human tissues with an average IC50 of 2.16 μM (0.12 μM~3.64 μM).
Mefuparib hydrochloride inhibits PARP3 (IC50>10 μM), PARP6 (IC50>10 μM), TNKS1 (IC50=1.6 μM), TNKS2 (IC50=1.3 μM).
In Vivo: Mefuparib hydrochloride (MPH; 40-160 mg/kg; orally; once every other day; for 21 days) displays dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group.
Mefuparib hydrochloride (160 mg/kg; orally; once every other day; for 21 days) inhibits the growth of the BR-05-0028 breast patient-derived xenograft (PDX) without obvious loss of body weight.
Mefuparib hydrochloride (10, 20, 40 mg/kg; oral) has a T1/2 of 1.07-1.3 hours and a C max of 116-725 ng/mL for SD rats.
Mefuparib hydrochloride (5, 10, 20 mg/kg; oral) has a T1/2 of 2.16-2.7 hours and a C max of 114-608 ng/mL for cynomolgus monkeys.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Children’s Drug Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | SY-5609 | BRD4 Inhibitor-18 | 8α-Tigloyloxyhirsutinolide 13-O-acetate | AAPK-25 | Dutasteride-13C6 | Oleic acid-13C | Anticancer agent 120 | Abacavir sulfate | Meloxicam-d3-1 | Thailanstatin D | SB-218078 | Toyocamycin | Sorafenib-d4 | Busulfan | PTC-028 | iRucaparib-AP6 | Dinaciclib | CR-1-31-B | 142I5 | Farudodstat | Ecteinascidin 770 | AT9283 | Staurosporine | SNS-032 | AZA1 | Antitumor agent-96 | Bleomycin A5 | Xevinapant | Mangiferin | Cambinol
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。