LDK-378 dihydrochloride

  • 化学数据
CAS号 1380575-43-8 货号 BCP10604
中文名 LDK-378 dihydrochloride
英文名 LDK-378 dihydrochloride
中文别名
英文别名 LDK 378;LDK378;Ceritinib;
分子式 C28H38Cl3N5O3S 分子量 631.06
  • 用途
生物活性 in vitro: LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells . in vivo: LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg .
信号通路 Angiogenesis/Protein Tyrosine Kinase 
靶 点 IGF1R ALK 

结构式

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