| Identification | Back Directory | [Name]
Takeda-6d | [CAS]
1125632-93-0 | [Synonyms]
CS-2670
Takeda-6d
TAKEDA 6D;TAKEDA6D
Benzamide, 2-chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)amino]thiazolo[5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]-
2-Chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)aMino][1,3]thiazolo[5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]benzaMide | [Molecular Formula]
C27H19ClFN5O3S | [MDL Number]
MFCD25977105 | [MOL File]
1125632-93-0.mol | [Molecular Weight]
547.99 |
| Hazard Information | Back Directory | [Biological Activity]
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. | [References]
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)
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