ALK-ROS1-IN-1-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Agonists • Screening Libraries www.MedChemE ALK/ROS1-IN-1 Cat. No.: HY-130794 CAS No.: 2365497-07-8 分⼦式: C₃₀H₃₅F₃N₆O₃ 分⼦量: 584.63 作⽤靶点: ALK; ROS 作⽤通路: Protein Tyrosine Kinase/RTK 储存⽅式: Please store the product under the recommended conditions in the COA. BIOLOGICAL ACTIVITY ⽣物活性 ALK/ROS1-IN-1 (compound 2e) 是⼀种⾼效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂，对 ALK 和 ROS1 酶作⽤的 I [1]C50 值分别为 0.174 μM 和 0.530 μM [1]。 IC50 Target IC50: 0.174 μM (ALK), 0.530 μM (ROS1) [1] 体外研究 ALK/ROS1-IN-1 displays potent anti-proliferative activity against ALK-addicted H3122 and ROS1-addicted HCC78 cell lines (IC50= 6.27 μM and 10.71 μM, respectively) [1]. ALK/ROS1-IN-1 shows impressive enzyme activity against clinically Crizotinib-resistant ALKL1196M with an IC50 value of 41.3 nM [1]. ALK/ROS1-IN-1 shows potent inhibitory activity in Ba/F3 cell line expressing ROS1 mutants, with IC50s of 137.7, 104.7 nM and 233.9 for wide-type, G2032R mutant and L2026M mutant, respectively [1].