Galunisertib (monohydrate)
Galunisertib monohydrate is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
Product Specifications
CAS Number
924898-09-9
UNSPSC
12352005
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/galunisertib-monohydrate.html
Smiles
O=C(C1=CC=C2N=CC=C(C3=C(CCC4)N4N=C3C5=NC(C)=CC=C5)C2=C1)N.O
Molecular Formula
C22H21N5O2
Molecular Weight
387.43
References & Citations
[1]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.|[2]Cong L, et al. Targeting the TGF-β receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim) . 2014 Sep;347 (9) :609-15.|[3]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|[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 3
Frequently Asked Questions
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