GFH018 | TGF-βRI inhibitor | Probechem Biochemicals

Chemical Structure : GFH018

GFH018 (GFH-018)

Catalog No.: PC-24588Not For Human Use, Lab Use Only.

GFH018 is a small molecule inhibitor of transforming growth factor-β receptor I (TGF-βRI, ALK5) inhibitor with IC50 of 40 nM, >60-fold selective over p38α MAPK.

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Biological Activity

GFH018 is a small molecule inhibitor of transforming growth factor-β receptor I (TGF-βRI, ALK5) inhibitor with IC50 of 40 nM, >60-fold selective over p38α MAPK.

GFH018 inhibits Treg cell differentiation.

GFH018 exhibits proliferation inhibition on NIH 3T3 cells with IC50 of 0.73 uM.

GFH018 inhibits the metastasis of breast cancer cells in vivo.

GFH018 demonstrates adequate ADME/PK profiles and moderate in vivo antitumor activity as a monotherapy in the H22 model, along with a synergistic effect in the CT26 model when combined with an anti-PD-L1 antibody.

GFH018 acts as a tumor microenvironment immunostimulant by regulating immune cells and inhibiting cancer-associated fibroblasts and angiogenesis.

Physicochemical Properties

M.Wt	385.43
Formula	C21H19N7O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-3-(6-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-[1,2,4]triazolo[1,5-a]pyridin-5-yl)acrylamide

References

1. Guo Y, et al. BMC Cancer. 2024 Apr 10;24(1):444.
2. Jiang T, et al. J Med Chem. 2025 Jun 12. doi: 10.1021/acs.jmedchem.5c00121.

GFH018 (GFH-018)

Biological Activity

Physicochemical Properties

References

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