Chemical Name: 4-[2-(6-Methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide. Alternate Names: LY2157299
TGFß receptor 1 inhibitor / Cancer immunotherapeutic
Molecular Weight:
369.43
Purity:
98%, NMR (Conforms)
Form:
White solid
CAS Number:
[700874-72-2]
Formula:
C22H19N5O
Application Notes:
Galunisertib is a TGF-B kinase (ALK5) antagonist.1 It stimulated hematopoiesis from primary myelodysplastic syndrome bone marrow specimens via downregulation of SMAD2 phosphorylation.2 It has been in clinical trials for treatment of various cancers.3-5 Galunisertib has more recently been used to enhance the anti-neuroblastoma activity of anti-GD2 antibody Dinutuximab with natural killer cells6 and preserved the function of in vitro expanded natural killer cells in AML and colon cancer models7. Galunisertib reversed TGF and regulatory T cell mediated suppression of human T cell proliferation. In combination with PD-L1 blockade, it resulted in improved tumor growth inhibition and complete regressions in colon carcinoma models.8
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