Galunisertib

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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