Figure 1. MPT0L145 inhibits FGFR signaling and exerts anti-growth effects on FGFR-activated cancer cell lines.

A. Synthesis of compound 1 (MPT0L145). Reagents and condition. (1) conc. HCl (aq.), H₂O, -78°C then POCl₃, DMF, DCM, 0°C to rt; (2) 2 M Methylamine in THF, IPA, rt; (3) 4-(4-Ethyl-piperazin-1-yl)-phenylamine, AcOH/H₂O, reflux; (4) 2,4,6-Trichloro-3,5-dimethoxy-phenylamine, triphosgene, p-dioxane, toluene, reflux then toluene, reflux. Abbreviations: DMF, N, N-dimethylformamide; DCM, dichloromethane; THF, tetrahydrofuran; IPA, isopropyl alcohol; AcOH, acetic acid. The details are described in Supplementary Methods. B. The anti-growth activity of MPT0L145 was examined in a panel of 15 cancer cell lines and normal HUVEC cells. Data are expressed as Log (IC₅₀/Mean IC₅₀). Black bar depicts cell lines in which FGFR signaling is reportedly activated. C. Effects of MPT0L145 on the viability of bladder cancer cells. RT-112, RT4 and T24 cells were treated with the indicated concentrations of MPT0L145 for 72 h. Cell viability was assessed the MTT assay. Data are expressed as means ± S.D. (***P < 0.001 compare to control group) D. MPT0L145 has less toxicity to normal cells. HUVECs were treated with indicated concentrations of MPT0L145 for 72 hours and viability was examined by MTT assay. Data are expressed as means ± S.D. (***P < 0.001 compare to control group)