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.