Galunisertib
CAS#: 700874-72-2
Description: Galunisertib, also known as LY2157299, is a novel selective small molecule transforming growth factor beta receptor (TGF-βR) kinase inhibitor. LY2157299 inhibited HCC cell migration on Laminin-5, Fibronectin, Vitronectin, Fibrinogen and Collagen-I and de novo phosphorylation of pSMAD2. LY2157299 inhibited HCC migration and cell growth independently of the expression levels of TGF-βRII.
Synonym: LY2157299; LY2157299; LY 2157299; Galunisertib
IUPAC/Chemical Name: 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide
THEORETICAL ANALYSIS
Name: LY2157299 (Galunisertib)
CAS#: 700874-72-2
Chemical Formula: C22H19N5O
Exact Mass: 369.15896
Molecular Weight: 369.41916
Elemental Analysis: C, 71.53; H, 5.18; N, 18.96; O, 4.33
TECHNICAL DATA
ADDITIONAL INFORMATION
LY2157299 is a novel selective small molecule transforming growth factor beta receptor (TGF-βR) kinase inhibitor. LY-2157299 could inhibit TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells. Furthermore, in vivo administration of LY-2157299 ameliorated anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure. Most importantly, treatment with LY-2157199 stimulated hematopoiesis from primary MDS bone marrow specimens. These studies demonstrate that reduction in SMAD7 is a novel molecular alteration in MDS that leads to ineffective hematopoiesis by activating of TGF-β signaling in hematopoietic cells. These studies also illustrate the therapeutic potential of TBRI inhibitors in MDS. (source: Cancer Res. 2011 Feb 1;71(3):955-63. Epub 2010 Dec 28. ).
REFERENCES
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