生物活性

• 靶点

  c-Kit IC50:7nM

  C-Raf IC50:2.5nM

  c-RET IC50:1.5nM

  PDGFRβ IC50:22nM

  VEGFR1 IC50:13nM

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• 描述Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KIT and RET, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner.
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  DLD1	1-20 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	25071018
  DLD1	1-10 μM	Apoptosis Assay	48 h	induces cell death in a dose-dependent manner	25071018
  DLD1	40 μM	Function Assay	24 h	induces PUMA protein and cell apoptosis	24763611

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• 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
  NCT02288078	Rectal Cancer	Phase 2	Unknown	September 2016	Japan ... more >> Saiseikai Fukuoka General Hospital Recruiting Fukuoka, Japan, 810-0001 Contact: Yasunori Emi, MD, PhD    +81-92-771-8151    emi-y@saiseikai-hp.chuo.fukuoka.jp Collapse <<
  NCT03347292	Carcinoma, Hepatocellular	Phase 1	Recruiting	February 17, 2021	United States, California ... more >> USC Norris Hospital and Clinics Recruiting Los Angeles, California, United States, 90033 United States, Florida H. Lee Moffitt Cancer Center & Research Institute Recruiting Tampa, Florida, United States, 33612 United States, New York Mount Sinai Medical Center Recruiting New York, New York, United States, 10029 United States, Washington Seattle Cancer Care Alliance Recruiting Seattle, Washington, United States, 98109-1023 Germany Universitätsklinikum Köln Not yet recruiting Köln, Nordrhein-Westfalen, Germany, 50937 Universitätsmedizin der Johannes Gutenberg Universität Mainz Not yet recruiting Mainz, Rheinland-Pfalz, Germany, 55131 Collapse <<
  NCT01187615	Small Cell Lung Carcinoma	Phase 1	Terminated	-	United States, Connecticut ... more >> New Haven, Connecticut, United States, 06519 United States, Nevada Las Vegas, Nevada, United States, 89135-3011 United States, New York New York, New York, United States, 10065 United States, North Carolina Chapel Hill, North Carolina, United States, 27599 Collapse <<

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