| Bioactivity | AXL-IN-14 is a potent and orally active AXL inhibitor with an IC50 value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity[1]. |
| Target | IC50: 0.8 nM (AXL) |
| Invitro | AXL-IN-14 (0.2, 1, 5 nM; 1 h) 以剂量依赖性方式降低 p-AXL 和 p-AKT 蛋白表达水平[1]。AXL-IN-14 (72 h) 显示抗增殖活性，对 EBC-1 细胞的 IC50 值为 21.8 nM[1]。AXL-IN-14 (20, 100 nM; 24 h) 抑制 H1299 和 SNU449 细胞中 Gas6/AXL 介导的细胞迁移和侵袭[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | AXL-IN-14 (1, 10 mg/kg; p.o.; once daily for 11 days) 在裸鼠体内显示出抗肿瘤活性[1]。 Animal Model: |
| Name | AXL-IN-14 |
| Formula | C32H24F2N4O4 |
| Molar Mass | 566.55 |
| 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]. Zhengsheng Zhan, et al. Discovery of 10H-Benzo[b]pyrido[2,3-e][1,4]oxazine AXL Inhibitors via Structure-Based Drug Design Targeting c-Met Kinase. J. Med. Chem. 2022. |