| Bioactivity | CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (Ki=3.1 μM) and VEGFR-2 (IC50=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) [1]. |
| Invitro | CA IX/VEGFR-2-IN-2 (compound 5e) 对反应性肿瘤细胞的选择性顺序是 PANC1，其次是 MCF7 和 PC3 并降低了 PANC1 细胞的迁移[1]。CA IX/VEGFR-2-IN-2 (compound 5e) 在胰腺癌细胞中诱导了 p53，BAX，细胞色素 C 和 caspases 3，8，9 表达的上调以及 Bcl-2 基因表达的下调引起细胞凋亡[1]。CA IX/VEGFR-2-IN-2 (compound 5e) 抑制 HIF-1α 表达从 6.1±0.13 ng/mL 降低到 3.7±0.09 ng/mL，抑制幅度超过 1.5 倍在 PANC1 细胞中[1]。CA IX/VEGFR-2-IN-2 (compound 5e) 引起 ROS 形成异常增加导致 PANC1 细胞周期停止或凋亡在 PANC1 细胞中[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CA IX/VEGFR-2-IN-2 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| In Vivo | CA IX/VEGFR-2-IN-2 (compound 5e) (5 和 10 mg/kg，腹腔注射，持续两周) 在雌性瑞士白化小鼠体内减少肿瘤体积和重量方面比标准药物 DOX (10 mg/kg) 更有效[1]。CA IX/VEGFR-2-IN-2 (compound 5e) (5 和 10 mg/kg，腹腔注射，持续两周) 对雌性瑞士白化小鼠注射 10 mg/kg 导致 VEGF， MMP-2 和 MMP-9 浓度的进一步降低[1]。CA IX/VEGFR-2-IN-2 (compound 5e) (5 和 10 mg/kg，腹腔注射，持续两周) 对雌性瑞士白化小鼠注射 5 mg/kg 导致坏死区域的形成， 并散布着不同的肿瘤细胞， 而在 10 mg/kg 的剂量下则有明显的改善， 肌肉束中的弥散性和广泛性坏死区域被取代， 肿瘤细胞的数量明显减少， 表明对活的肿瘤细胞有实质性的抑制[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C22H18FN3O3S |
| Molar Mass | 423.46 |
| 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]. Hefny S M, et al. Discovery and Mechanistic Studies of Dual-Target Hits for Carbonic Anhydrase IX and VEGFR-2 as Potential Agents for Solid Tumors: X-ray, In Vitro, In Vivo, and In Silico Investigations of Coumarin-Based Thiazoles[J]. Journal of Medicinal Chemistry, 2024. |