| Bioactivity | ALK/ROS1-IN-5 (compound X4) is a selective ALK and ROS1 kinases inhibitor with IC50s of 0.512 μM (ALK), 0.766 μM (ROS1), respectively. ALK/ROS1-IN-5 inhibits H2228 cells with an IC50 of 0.034 μM. ALK/ROS1-IN-5 induces cancer cells apoptosis in dose-dependent manner. ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells[1]. |
| Invitro | ALK/ROS1-IN-5 (0-100 μM, 72 h) 对 H2228，H1975 和 H460 细胞均具有优异的抑制活性[1]。ALK/ROS1-IN-5 (10 μM) 对酪氨酸激酶家族成员，包括 EGFR，AKT1，FGFR1 和 ERK1 具有显著抑制活性[1]。ALK/ROS1-IN-5 (10 μM) 对 ALK 和 ROS1 具有明显的激酶抑制活性，抑制率分别为 94.34% 和94.27%[1]。ALK/ROS1-IN-5 (1-2 μM, 24 h) 剂量依赖性地抑制 H2228 细胞迁移[1]。ALK/ROS1-IN-5 (1-2 μM, 24 h) 剂量依赖性地诱导 H2228 细胞凋亡和细胞周期阻滞[1]。ALK/ROS1-IN-5 (0.1- 0.5 μM, 24 h) 以剂量依赖性方式降低 ALK 和 ERK 的磷酸化。[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ALK/ROS1-IN-5 相关抗体: Cell Cycle Analysis [1] Cell Line: |
| In Vivo | ALK/ROS1-IN-5 (60, 120 mg/kg, p.o., daily, 7 days) 对小鼠血液生化样品无明显毒性[1]。ALK/ROS1-IN-5 (10 mg/kg, p.o., daily, 35 days) 显示出良好的抗肿瘤作用[1]。ALK/ROS1-IN-5 (5-25 mg/kg, p.o., daily, 14 days) 对网织红细胞减少的影响最小[1]。ALK/ROS1-IN-5 (25-50 mg/kg, p.o., daily, 21 days) 药物组的肿瘤体积生长率低于阳性对照组[1]。ALK/ROS1-IN-5 以剂量依赖的方式降低 Ki67，Bcl2，Caspase 3 和 PCNA[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C32H28F2N4O3 |
| Molar Mass | 554.59 |
| 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]. Huang X, et al. Revealing 5-(3,5-difluorobenzyl)-1H-indazole as the active pharmacophore of ALK/ROS1 dual inhibitors through theoretical calculations and biological activity evaluations. Bioorg Chem. 2025 Jan;154:108014. |