Galunisertib

Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.

Product Specifications

CAS Number

[700874-72-2]

Product Name Alternative

LY2157299

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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/LY2157299.html

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=CC=CC(C2=NN3C(CCC3)=C2C4=CC=NC5=C4C=C(C=C5)C(N)=O)=N1

Molecular Formula

C22H19N5O

Molecular Weight

369.42

Precautions

H302, H315, H319, H335

References & Citations

[1]Cong L, et al. Targeting the TGF-β receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim) . 2014 Sep;347 (9) :609-15.|[2]Serova M, et al. Effects of TGF-beta signalling inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. Oncotarget. 2015 Aug 28;6 (25) :21614-27|[3]Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44 (1) :142-50.|[4]Herbertz S, et al. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway. Drug Des Devel Ther. 2015 Aug 10;9:4479-99.