LY-364947
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II[1].
Product Specifications
CAS Number
[396129-53-6]
Product Name Alternative
HTS466284
UNSPSC
12352005
Hazard Statement
H301, H315, H319, H335, H400
Target
TGF-β Receptor
Type
Reference compound
Related Pathways
TGF-beta/Smad
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/LY-364947.html
Purity
99.23
Solubility
DMSO : 15.62 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
C1(C2=CNN=C2C3=NC=CC=C3)=CC=NC4=CC=CC=C14
Molecular Formula
C17H12N4
Molecular Weight
272.30
Precautions
H301, H315, H319, H335, H400
References & Citations
[1]Peng SB, et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry, 2005, 44 (7), 2293-2304.|[2]Oka M, et al. Inhibition of endogenous TGF-beta signaling enhances lymphangiogenesis. Blood, 2008, 111 (9), 4571-4579.|[3]Naka K, et al. TGF-beta-FOXO signalling maintains leukaemia-initiating cells in chronic myeloid leukaemia. Nature, 2010, 463 (7281), 676-680.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Curated Selection
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