生物活性

• 描述CH5424802 hydrochloride is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03498521	Cancer of Unknown Primary Site	Phase 2	Recruiting	April 16, 2022	-
  NCT02013219	Non-Small Cell Lung Cancer	Phase 1	Active, not recruiting	January 18, 2019	United States, California ... more >> UC Irvine Medical Center Orange, California, United States, 92868 United States, Connecticut Yale University School Of Medicine New Haven, Connecticut, United States, 06510 United States, Florida Florida Hospital Cancer Inst Orlando, Florida, United States, 32804 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Massachusetts Massachusetts General Hospital;Hematology/ Oncology Boston, Massachusetts, United States, 02114 Beth Israel Deaconess Med Ctr; Neurology/MS Center Boston, Massachusetts, United States, 02215 Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, Michigan Karmanos Cancer Center; Department of Oncology Detroit, Michigan, United States, 48201 United States, New York Memorial Sloan Kettering - Basking Ridge New York, New York, United States, 10065 United States, Ohio Case Western Reserve University; Medicine-Hematology and Oncology Cleveland, Ohio, United States, 44106 United States, South Carolina Greenville Health System Greenville, South Carolina, United States, 29605 France Institut Gustave Roussy Villejuif, France, 94805 Hong Kong The Chinese University of Hong Kong Shatin, Hong Kong, 123456 Korea, Republic of Seoul National University Hospital Seoul, Korea, Republic of, 03080 Asan Medical Center Seoul, Korea, Republic of, 05505 Spain START Madrid. Centro Integral Oncologico Clara Campal; CIOCC Madrid, Spain, 28050 Hospital Clinico Universitario de Valencia Valencia, Spain, 46010 United Kingdom Queen Mary University of London London, United Kingdom, EC1M 6BQ Collapse <<
  NCT01801111	Non-Small-Cell Lung Carcinoma	Phase 1 Phase 2	Completed	-	-

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• 参考文献

• [1] Kinoshita K, Asoh K, et al. Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802). Bioorg Med Chem. 2012 Feb 1;20(3):1271-80.

  [2] Sakamoto H, Tsukaguchi T, et al. CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant. Cancer Cell. 2011 May 17;19(5):679-90.