ALK/ROS1-IN-1 

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC₅₀s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

IC50: 0.174 μM (ALK), 0.530 μM (ROS1)^[1]

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 ALK^L1196M 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].
ALK/ROS1-IN-1 has no significant effect on inducing apoptosis of HCC78 cell line^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

584.63

C₃₀H₃₅F₃N₆O₃

2365497-07-8

O=C([C@H]1CCCN(C2=CC(NC3=CC=C(N4CCNCC4)C=C3OC)=NC=C2)C1)NCC5=CC=C(OC(F)(F)F)C=C5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu S, et al. Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors. Eur J Med Chem. 2019 Oct 1;179:358-375.  [Content Brief]