Takeda-6d |
| Catalog No.GC49700 |
Takeda-6D (composé 6d) est un inhibiteur puissant et actif par voie orale de BRAF/VEGFR2, avec des valeurs IC50 de 7,0 et 2,2 nM, respectivement. Takeda-6D montre une antiangiogenèse en supprimant la voie VEGFR2 dans les cellules HUVEC stimulées par 293/KDR et VEGF. Takeda-6D montre une suppression significative de la phosphorylation de ERK1/2. Takeda-6D montre une activité antitumorale.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1125632-93-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Takeda-6d is a dual inhibitor of RAF kinases and VEGFR2.1 It inhibits wild-type B-RAF, mutant B-RAFV600E, and C-RAF (IC50s = 12, 7, and 1.5 nM, respectively), as well as VEGFR2 (IC50 = 2.8 nM). Takeda-6d is selective for these kinases over a panel of 19 additional kinases (IC50s = >1,000 nM) but does inhibit FGFR3, PDGFRα, and PDGFRβ (IC50s = 22, 12, and 5.5 nM, respectively). It inhibits MEK and ERK1/2 phosphorylation in several colon cancer and melanoma cell lines expressing B-RAFV600E when used at concentrations ranging from 100 to 1,600 nM, as well as inhibits VEGF-A-induced phosphorylation of VEGFR2 in VEGFR2-overexpressing KDR cells (IC50 = 0.53 nM). Takeda-6d (10 mg/kg) reduces tumor volume in an A375 melanoma mouse xenograft model.
1.Okaniwa, M., Hirose, M., Imada, T., et al.Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffoldsJ. Med. Chem.55(7)3452-3478(2012)
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *