Galunisertib

Biological Activity

Galunisertib is an ALK4 and ALK5 (TGFβRI) inhibitor (IC₅₀ values are 77.7 and 172 nM, respectively). Also inhibits a range of other kinases with submicromolar IC₅₀s including MINK, TGFβRII, ALK6 and ACVR2B. Inhibits TGFβ-induced SMAD phosphorylation in cancer cell lines in vitro and in vivo. Also reverses TGFβ-mediated suppression of T cell proliferation. Prevents TGFβ-mediated EMT and cell migration in vitro and exhibits antitumor efficacy in vivo. Used as component of growth media for urothelial organoids. Orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
   Yingling et al.
   Oncotarget, 2017;9:6659
2. Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade.
   Holmgaard et al.
   J.Immunother.Cancer., 2018;6:47
3. Urothelial organoids originating from Cd49f^high mouse stem cells display Notch-dependent differentiation capacity.
   Santos et al.
   Nat.Commun., 2019;10:4407

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