FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.

FGFR:0.106 μM, FGFR1:0.026 μM, PDGFRβ:0.077 μM, VEGFR2:0.025 μM

FGFR1/VEGFR2-IN-2 在 10 μM 浓度下显示出抗肿瘤细胞增殖活性，平均 GI 值达到 60.38%。该化合物对乳腺癌细胞系 T-47D、MCF-7 与 MDA-MB-231 表现出显著的细胞毒性，而对正常细胞 Vero 无明显影响。在 10 μM 和 20 μM 的浓度下，FGFR1/VEGFR2-IN-2 能有效阻止 T-47D 细胞在 G1 期的进程。此外，该化合物在 2.12 μM 和 4.25 μM 的浓度下激活了 T-47D 细胞的早期及晚期细胞凋亡并促进了细胞坏死过程。在 3.7 μM 至 4.8 μM 的浓度范围内，FGFR1/VEGFR2-IN-2 提升了 BAX 与 Caspase-3 的表达并下调了 BCL-2 的表达，进一步增强细胞坏死。此外，在 6 μM 浓度下，经过 24 小时与 48 小时处理后，FGFR1/VEGFR2-IN-2 对 T-47D 细胞展示了抗迁移特性。