ALK-IN-6 is an orally bioavailable inhibitor of anaplasticlymphomakinase (ALK, IC50s: 71 nM, 18.72 nM, and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L).
ALK-IN-12 is a highly potent and orally active inhibitor of anaplasticlymphomakinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.
Negative control for TL 13-112 . Displays no degradation of ALK in cell lines. Highly potent ALK inhibitor (IC50 = 0.34 nM). Powell et al (2018) Chemically induced degradation of anaplasticlymphomakinase. J.Med.Chem. 61 4249 PMID:29660984
Negative control for TL 13-12 . Displays no degradation of ALK in cell lines. Highly potent inhibitor of ALK (IC50 = 0.54 nM) Powell et al (2018) Chemically induced degradation of anaplasticlymphomakinase (ALK). J.Med.Chem. 61 4249 PMID:29660984
PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplasticlymphomakinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).