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Description: ALK4 and ALK5 (TGFβRI) inhibitor
Alternative Names: LY 2157299
Chemical Name: 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide
Purity: ≥98% (HPLC)
Citations (2)
Literature (3)
Pathways (1)

Biological Activity for Galunisertib

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.

Compound Libraries for Galunisertib

Galunisertib is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for Galunisertib

M. Wt 369.43
Formula C22H19N5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 700874-72-2
PubChem ID 10090485
Smiles CC1=NC(C2=NN3CCCC3=C2C4=CC=NC5=C4C=C(C(N)=O)C=C5)=CC=C1

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.

Solubility Data for Galunisertib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 36.94 100
ethanol 7.39 20

Preparing Stock Solutions for Galunisertib

The following data is based on the product molecular weight 369.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.71 mL 13.53 mL 27.07 mL
5 mM 0.54 mL 2.71 mL 5.41 mL
10 mM 0.27 mL 1.35 mL 2.71 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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References for Galunisertib

References are publications that support the biological activity of the product.

Yingling et al (2017) Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor. Oncotarget 9 6659 PMID: 29467918

Holmgaard et al (2018) 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. J.Immunother.Cancer. 6 47 PMID: 29866156

Santos et al (2019) Urothelial organoids originating from Cd49fhigh mouse stem cells display Notch-dependent differentiation capacity. Nat.Commun. 10 4407 PMID: 31562298

If you know of a relevant reference for Galunisertib, please let us know.

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Keywords: Galunisertib, Galunisertib supplier, TGFbetaRI, TGFBRI, inhibitors, inhibits, ALK5, ALK4, smad, phosphorylation, anticancer, orally, bioavailable, growth, media, organoids, LY, 2157299, TGF-beta, Receptors, Organoids, 6956, Tocris Bioscience

2 Citations for Galunisertib

Citations are publications that use Tocris products. Selected citations for Galunisertib include:

Natani et al (2022) Activation of TGF-β - SMAD2 signaling by IL-6 drives neuroendocrine differentiation of prostate cancer through p38MAPK. Cell Signal 91 110240 PMID: 34986386

David C et al (2020) A systems approach delivers a functional microRNA catalog and expanded targets for seizure suppression in temporal lobe epilepsy. Proc Natl Acad Sci U S A 117 15977-15988 PMID: 32581127

Do you know of a great paper that uses Galunisertib from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

  • Self-renewal and Maintenance
  • Differentiation
  • Reprogramming
  • Organoid Generation
  • GMP and Ancillary Material Grade Products
Stem Cells Scientific Review

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Stem Cells Poster

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for Galunisertib

TGF-β Signaling Pathway

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.