Chemical Name: 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide
Biological ActivityALK4 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.
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.
Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Yingling et al.
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.
Urothelial organoids originating from Cd49fhigh mouse stem cells display Notch-dependent differentiation capacity.
Santos et al.
No product specific FAQs exist for this product, however you mayView all Small Molecule FAQs
Reviews for Galunisertib
There are currently no reviews for this product. Be the first to review Galunisertib and earn rewards!
Have you used Galunisertib?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image