Formulation: A solid
Formal Name: 2-chloro-3-(1-cyanocyclopropyl)-N-[5-[[2-[(cyclopropylcarbonyl)amino][5,4-b]pyridin-5-yl]oxy]-2-fluorophenyl]-benzamide
Purity: ≥95%
Formula Markup: C27H19ClFN5O3S
Formula Weight: 548
Shelf life (days): 1460
CAS Number: 1125632-93-0
Notes: Takeda-6d is a dual inhibitor of RAF kinases and VEGFR2.{61875} 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.
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