|
|
| | FGFR-IN-13 Basic information |
| Product Name: | FGFR-IN-13 | | Synonyms: | FGFR-IN-13;2-Propenamide, N-[4-[[6-(3,5-dimethoxyphenyl)-9H-purin-9-yl]methyl]phenyl]- | | CAS: | 2962941-25-7 | | MF: | C23H21N5O3 | | MW: | 415.45 | | EINECS: | | | Product Categories: | | | Mol File: | 2962941-25-7.mol |  |
| | FGFR-IN-13 Chemical Properties |
| density | 1.27±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | | pka | 13.41±0.70(predicted) |
| | FGFR-IN-13 Usage And Synthesis |
| Uses | 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 |
| | FGFR-IN-13 Preparation Products And Raw materials |
|