Bioactivity | Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy[1]. |
Invitro | Axl-IN-17 在1 μM 的浓度下可以抑制 TYRO3,MER,MET,RON 等多种激酶[1]。Axl-IN-17 在 BaF3/TEL-AXL 细胞中展现出抗增殖活性,IC50 值<1 nM[1]。Axl-IN-17 (1 nM,2 h) 抑制 AXL 磷酸化和其下游信号通路[1]。 0 --> Axl-IN-17 相关抗体: Cell Proliferation Assay[1] Cell Line: |
In Vivo | Axl-IN-17 (口服,3 mg/kg,每天一次)具有良好的药代动力学特性,半衰期是10.09 小时,AUC 值是59815 ng•h/mL[1]。Axl-IN-17(p.o.,25,50,100 mg/kg,每天一次,共七天)在 AXL 驱动的肿瘤异种小鼠中表现出抗肿瘤效应[1]。AXL-IN-17在雄性Sprague-Dawley鼠体内的药代动力学分析[1]Route |
Name | Axl-IN-17 |
Formula | C32H27F2N7O |
Molar Mass | 563.60 |
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]. Lan Y,et al., Discovery of a 1,6-naphthyridin-4-one-based AXL inhibitor with improved pharmacokinetics and enhanced in vivo antitumor efficacy. Eur J Med Chem. 2024 Feb 5;265:116045. |