生物活性

• 描述Dabrafenib mesylate is a potent, and selective Raf kinase inhibitor that is capableof inhibiting the kinase activity of B-Raf^V600E and c-Raf with IC₅₀ values of 0.6 nM and 5.0 nM, respectively.
• 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
  NCT02416232	-	-	-	-	France ... more >> GSK Investigational Site Amiens Cedex, France, 80054 GSK Investigational Site Angers, France, 49100 GSK Investigational Site Bayonne cedex, France, 64109 GSK Investigational Site Besancon cedex, France, 25030 GSK Investigational Site Bobigny, France, 93000 GSK Investigational Site Bordeaux, France, 33075 GSK Investigational Site Boulogne-Billancourt, France, 92100 GSK Investigational Site Brest cedex, France, 29609 GSK Investigational Site Caen Cedex 9, France, 14033 GSK Investigational Site Chambray-Les-Tours, France, 37170 GSK Investigational Site Clermont-Ferrand cedex 1, France, 63003 GSK Investigational Site Creteil, France, 94010 GSK Investigational Site Dijon Cedex, France, 21079 GSK Investigational Site Grenoble cedex 9, France, 38043 GSK Investigational Site La Rochelle cedex 1, France, 17019 GSK Investigational Site Le Havre, France, 76083 GSK Investigational Site Le Mans, France, 72000 GSK Investigational Site Lille, France, 59037 GSK Investigational Site Limoges cedex, France, 87042 GSK Investigational Site Lorient, France, 56322 GSK Investigational Site Lyon Cedex 08, France, 69373 GSK Investigational Site Marseille Cedex 5, France, 13385 GSK Investigational Site Montpellier cedex 5, France, 34295 GSK Investigational Site Montpellier Cedex 5, France, 34298 GSK Investigational Site Mulhouse, France, 68100 GSK Investigational Site Nantes Cedex 1, France, 44093 GSK Investigational Site Nice, France, 06202 GSK Investigational Site Nimes, France, 30029 cedex 9 GSK Investigational Site Orleans Cedex 2, France, 45067 GSK Investigational Site Paris Cedex 10, France, 75475 GSK Investigational Site Paris, France, 75006 GSK Investigational Site Pau, France, 64000 GSK Investigational Site Pierre-Benite cedex, France, 69495 GSK Investigational Site Poitiers, France, 86021 GSK Investigational Site Pringy Cedex, France, 74374 GSK Investigational Site Reims Cedex, France, 51092 GSK Investigational Site Rennes Cedex, France, 35042 GSK Investigational Site Rouen, France, 76031 GSK Investigational Site Saint-Pierre, France, 97448 GSK Investigational Site Saint-Priest en Jarez, France, 42270 GSK Investigational Site Strasbourg Cedex, France, 67091 GSK Investigational Site Thionville, France, 57126 Cedex 1 GSK Investigational Site Toulouse Cedex 9, France, 31059 GSK Investigational Site Valence Cedex 9, France, 26953 GSK Investigational Site Vandoeuvre-Les-Nancy, France, 54511 GSK Investigational Site Villejuif cedex, France, 94805 Collapse <<
  NCT01682083	Melanoma	Phase 3	Active, not recruiting	November 30, 2030	-
  NCT01682083	-	-	Active, not recruiting	-	-

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• 参考文献

• [1] Lee S, Ku SK, Bae JS. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Aug 25;256:266-73.

  [2] Greger JG, Eastman SD, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11(4):909-20.