| Bioactivity | FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells[1]. |
| Invitro | FGFR1/VEGFR2-IN-2 (10 μM) 具有抗肿瘤增殖活性，平均 GI 为 60.38%[1]。FGFR1/VEGFR2-IN-2 对乳腺癌细胞系 T-47D，MCF-7 和 MDA-MB-231 有较好的细胞毒性，对正常细胞 Vero 没有影响[1]。FGFR1/VEGFR2-IN-2 (10，20 μM) 将 T-47D 细胞阻滞在 G1 期[1]。FGFR1/VEGFR2-IN-2 (2.12，4.25 μM) 促进 T-47D 细胞早期和晚期细胞凋亡，促进细胞坏死[1]。FGFR1/VEGFR2-IN-2 (3.7-4.8 μM) 促进细胞坏死，提高了 BAX 和 Caspase-3 的表达，降低了 BCL-2 的表达[1]。FGFR1/VEGFR2-IN-2 (6 μM；24，48 h) 在 T-47D 中有抗迁移作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> FGFR1/VEGFR2-IN-2 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| Formula | C21H15ClF3NO4S |
| Molar Mass | 469.86 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Rasha M Hassan, et al. Novel benzenesulfonamides as dual VEGFR2/FGFR1 inhibitors targeting breast cancer: Design, synthesis, anticancer activity and in silico studies. Bioorg Chem. 2024 Aug 17:152:107728. |