| Bioactivity | VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells[1]. |
| Invitro | VEGFR-2/AKT-IN-2 具有与索拉非尼 (HY-10201) 相似的 VEGFR2 抑制活性，IC50 为 0.061 μM[1]。VEGFR-2/AKT-IN-2 (0.39-100 μM, 48 h) 抑制 HepG-2 和 HuH-7 细胞系生长，其 IC50 值分别为 0.75 和 3.43 μM[1]。VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) 减少 HepG-2 细胞中总的和磷酸化的 AKT[1]。VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) 促进细胞凋亡，增加早期和晚期凋亡细胞占比 (分别从0.39%增加到26.28%，从0.21%增加到18.87%)，上调 BAX 和 caspase-3，下调 Bcl-2[1]。VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) 阻止 HepG-2 细胞在 S 期的细胞周期进展[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> VEGFR-2/AKT-IN-2 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| Formula | C25H16FN5S |
| Molar Mass | 437.49 |
| 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]. Abusaif, et al. Exploring a novel thiazole derivatives hybrid with fluorinated-indenoquinoxaline as dual inhibitors targeting VEGFR2/AKT and apoptosis inducers against hepatocellular carcinoma with docking simulation. Bioorganic chemistry. 2024, 154, 108023. |