LY2109761

LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.

Product Specifications

CAS Number

[700874-71-1]

UNSPSC

12352005

Hazard Statement

H302

Target

Autophagy; TGF-β Receptor

Type

Reference compound

Related Pathways

Autophagy; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LY2109761.html

Purity

99.72

Solubility

DMSO : 6.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N12N=C(C(C3=C4C=CC(OCCN5CCOCC5)=CC4=NC=C3)=C1CCC2)C6=NC=CC=C6

Molecular Formula

C26H27N5O2

Molecular Weight

441.52

Precautions

H302

References & Citations

[1]Melisi D, et al. LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol Cancer Ther, 2008, 7 (4), 829-840.|[2]Fransvea E, et al. Blocking transforming growth factor-beta up-regulates E-cadherin and reduces migration and invasion of hepatocellular carcinoma cells. Hepatology, 2008, 47 (5), 1557-1566.|[3]Zhang M, et al. Blockade of TGF-β signaling by the TGFβR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma. Cancer Res, 2011, 71 (23), 7155-7167.