BI-4659
BI-4659 (Compound 47i) is a TGF-β type I receptor (TGF-βRI) (Alk5) inhibitor with an IC50 of 19 nM. BI-4659 also inhibits (IC50: 99 nM) and significantly blocks TGFβRI-mediated phosphorylation of Smad2/3 with low cross-reactivities within the human kinome. BI-4659 can be used for fibrotic diseases like idiopathic pulmonary fibrosis (IPF) and cancers research[1].
Product Specifications
CAS Number
894784-05-5
UNSPSC
12352005
Target
PDGFR; TGF-beta/Smad; TGF-β Receptor
Related Pathways
Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad
Field of Research
Cancer; Inflammation/Immunology
Smiles
CN(C)CC(C=C1)=CC=C1N/C(C2=CC=CC=C2)=C3C4=CC=C(C(NCC)=O)C=C4NC/3=O
Molecular Formula
C27H28N4O2
Molecular Weight
440.54
References & Citations
[1]Roth GJ, et al. Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor I (TGFβRI) . J Med Chem. 2010 Oct 28;53 (20) :7287-95.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
ALK5; PDGFRα
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