Pimasertib

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  |  Serine/Threonine Kinase Inhibitor Library  |  Trametinib  |  PD98059  |  Mirdametinib  |  U0126-EtOH  |  Selumetinib  |  Cobimetinib  |  Binimetinib  |  C16-PAF  |  Isorhamnetin  |  Lidocaine  |  Avutometinib  |  BIX02189  |  CI-1040  |  trans-Zeatin  |  Refametinib  |  GDC-0623  |  MS432  |  TAK-733  |  AZD8330  |  BI-847325  |  APS-2-79  |  RGB-286638  |  SL327  |  GW284543  |  RO4987655  |  Lixisenatide

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

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds