GFH018 | TGF-βRI inhibitor | Probechem Biochemicals

Chemical Structure : GFH018

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GFH018 (GFH-018)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	385.43
分子式	C21H19N7O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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)

生物&药学活性

物理化学性质&存储条件

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GFH018 (GFH-018)

生物&药学活性

物理化学性质&存储条件

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