Galunisertib (LY2157299), TGFB kinase antagonist

Key facts

CAS number

700874-72-2

Purity

>98%

Form

Solid

form

Molecular weight

369.4 Da

Molecular formula

C₂₂H₁₉N₅O

PubChem

10090485

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Biochemical name

Galunisertib

Biological description

Highly potent, TGF-beta kinase (ALK5) inhibitor (IC₅₀ = 56 nM). Downregulates Smad2 phosphorylation. Increases VEGF-induced HUVEC cell migration. Enhances anti-neuroblastoma activity of Dinuxtuximab (anti-GD2 antibody) with natural killer cells. Reverses supression of human T cell proliferation induced by TGF-beta and regulatory T cells. Improves tumour growth inhibition and regression in colon carcinoma models. ALK4 and ALK5 (TGFβRI) inhibitor; component of growth media for urothelial organoids.

Canonical smiles

CC1=NC(=CC=C1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(=O)N

InChi

InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)

InChiKey

IVRXNBXKWIJUQB-UHFFFAOYSA-N

IUPAC Name

4-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide