Galunisertib

Name: Galunisertib
Brand: Tocris Bioscience
SKU: 6956

Tocris Bioscience, part of Bio-Techne | Catalog # 6956

Citations (8)

COA / SDS

ALK4 and ALK5 (TGFβRI) inhibitor

Key Product Details

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)
Molecular Weight:	369.43

View Full Technical Details for Galunisertib

Technical Data
Citations

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
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 for Galunisertib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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.

Holmgaard 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. 2018 PMID: 29866156
Santos Urothelial organoids originating from Cd49f^high mouse stem cells display Notch-dependent differentiation capacity. Nat.Commun. 2019 PMID: 31562298
Yingling Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor. Oncotarget 2017 PMID: 29467918