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FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity[1]. | [in vivo]
FGFR-IN-13 (10 and 30 mg/kg, po; everyday for 21 days) inhibits tumor growth in a dose-dependent manne. FGFR-IN-13 has a favorable safety profile and is effective in inhibiting tumor growth at safe doses in MDA-MB-231 xenograft tumor mouse mode[1]. | Animal Model: | MDA-MB-231 xenograft tumor mouse model[1] | | Dosage: | 10 and 30 mg/kg | | Administration: | Oral gavage (p.o.) | | Result: | Did not cause significant weight loss.
Achieved tumor growth inhibition (TGI) of 64.21% at high doses (30 mg/kg).
Achieved tumor growth inhibition (TGI) of 40.22% at low doses (10 mg/kg). |
| [References]
[1] Wang Y, et al. Discovery of N-(4-((6-(3, 5-Dimethoxyphenyl)-9H-Purine Derivatives as Irreversible Covalent FGFR Inhibitors[J]. European Journal of Medicinal Chemistry, 2024: 116415. DOI:10.1016/j.ejmech.2024.116415 |
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