Galunisertib

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Cat.No. 6956 - Galunisertib | C22H19N5O | CAS No. 700874-72-2
Description: ALK4 and ALK5 (TGFβRI) inhibitor
Chemical Name: 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

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. Orally bioavailable.

Technical Data

M. Wt 369.43
Formula C22H19N5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 700874-72-2
PubChem ID 10090485
InChI Key IVRXNBXKWIJUQB-UHFFFAOYSA-N
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

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

Preparing Stock Solutions

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.

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

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


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

Citations for Galunisertib

Citations are publications that use Tocris products.

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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* or download your copy today!

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


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Stem Cells

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

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

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.