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。

Pimasertib

CAS No. : 1236699-92-5

MCE 国际站：Pimasertib

产品活性：Pimasertib (AS703026) 是一种高效，具有选择性，口服活性的、ATP 非竞争性的 MEK1/2 别构抑制剂，主要用于癌症研究。

研究领域：MAPK/ERK Pathway

作用靶点：MEK

In Vitro: Pimasertib (5, 0.5, and 0.1 μM) specifically blocks ERK1/2 activation in MM cells, cultured alone or with BMSCs. Pimasertib inhibits the growth of MM cell lines in a dose-dependent manner, with IC₅₀s ranging from 0.005 to 2 μM. The IC₅₀s of Pimasertib against INA-6, U266, H929 cells are 10 nM, 5 nM, 200 nM respectively. Pimasertib induces apoptosis and modulates the cell cycle profile. Pimasertib targets MM cells in the BM microenvironment. Pimasertib (10 μmol/L) inhibits ERK pathway, proliferation, and transformation in cetuximab-resistant D-MUT cells. Pimasertib in combination with PLX4032 significantly induces apoptosis of RPMI-7951 cells, whereas each drug used alone does not. Pimasertib synergizes with small interfering RNA-mediated downregulation of BRAF to produce results similar to those of combined treatment with PLX4032 and Pimasertib.

In Vivo: Pimasertib (15, 30 mg/kg) significantly inhibits the growth of tumor in the human H929 MM xenograft model in CB17 SCID mice. Pimasertib (10 mg/kg, p.o.) inhibits tumor growth of cetuximab-resistant tumor attributed by K-ras mutation.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  MAPK Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Ferroptosis Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Obesity Compound Library  |  Angiogenesis-Related Compound Library  |  Targeted Diversity Library  |  Anti-Liver Cancer Compound Library   |  Rare Diseases Drug Library  |  Anti-Colorectal Cancer Compound Library   |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Highly Selective Inhibitors Library  |  Avutometinib  |  Cobimetinib racemate  |  Trametinib (DMSO solvate)  |  PD184161  |  MEK-IN-6  |  GW284543 hydrochloride  |  trans-Zeatin-d₅  |  BI-847325  |  Hypothemycin  |  Debromohymenialdisine  |  RGB-286638  |  Binimetinib  |  Trametinib-d₄  |  Gossypetin  |  Lidocaine-d₁₀ hydrochloride  |  Isorhamnetin  |  MS432  |  MEK1/2-IN-2  |  Trametinib-¹³C₆  |  MEK-IN-5  |  Lidocaine hydrochloride hydrate  |  PD 198306  |  CI-1040  |  (R)-PD 0325901CL  |  MEK/PI3K-IN-1  |  GDC-0623  |  N-Oxide Lidocaine-d₁₀

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。