GFH018 is a TGF-βR1 Inhibitor. GFH018 exhibited high selectivity against p38α and good target inhibitory activity. Additionally, GFH018 displayed favorable in vitro ADME and pharmacokinetic profiles across species. In murine tumor mouse models, either the monotherapy of GFH018 or the combination with an anti-PD-L1 antibody suppressed tumor growth, and potent inhibition of cancer cell migration in vivo was observed. Mechanistic studies revealed that GFH018 not only reactivated the immune system by blocking Treg- and M2macrophage-mediated immunosuppression but also inhibited tumor vascular angiogenesis
MedKoo Cat#: 129055
Name: GFH018
CAS#: 2169299-67-4
Chemical Formula: C21H19N7O
Exact Mass: 385.1700
Molecular Weight: 385.43
Elemental Analysis: C, 65.44; H, 4.97; N, 25.44; O, 4.15
The following data is based on the product molecular weight 385.43 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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3: Jiang T, Ge M, Liang T, Cai L, Yu X, Xie F, Wang L, Zhang J, Zhou F, Lu Q,
Lan J. Discovery of a Selective, Novel TGF-βR1 Inhibitor GFH018 for the
Treatment of Solid Tumors. J Med Chem. 2025 Jun 12. doi:
10.1021/acs.jmedchem.5c00121. Epub ahead of print. PMID: 40505138.
4: Jorna FH, Tobé TJ, Huisman RM, de Jong PE, Plukker JT, Stegeman CA. Early
identification of risk factors for refractory secondary hyperparathyroidism in
patients with long-term renal replacement therapy. Nephrol Dial Transplant. 2004
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