Repotrectinib is a potent ROS1 and TRK Inhibitor
Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. The IC50 values are 0.83/0.05/0.1 nM for TRKA/B/C, respectively. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib inhibits mutant ALKs. It inhibits ALK G1202R with an IC50 of 1.26 nM. Besides, it inhibits ALK L1196M with an IC50 of 1.08 nM)....
Crizotinib is an Orally Active, ATP-Competitive ALK and c-Met inhibitor
In this article, we will introduce an orally bioavailable, ATP-competitive ALK and c-Met inhibitor, Crizotinib. The IC50 values for ALK and c-Met kinases are 20 and 8 nM, respectively. Additionally, in cell-based assays, Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM, respectively. In...
LDN193189 is a Selective BMP Type I Receptor Inhibitor
Fibrodysplasia ossificans progressiva (FOP) is a congenital disorder of progressive. It is widespread postnatal ossification of soft tissues and is without known effective treatments. A recent study identified heterozygous mutations in ACVR1, the gene encoding the BMP type I receptor ALK2, in all affected members from seven families. BMP...
CJ-2360 is a Potent and Orally Active ALK Inhibitor
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor (IR) kinase superfamily. It highly expresses in adult brain tissue and exerts an important role in the development of the nervous system. Deregulation of ALK originally presents by the identification of at (2;5) chromosomal translocation...
TL13-12 is a Selective ALK-PROTAC Degrader
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase. ALK is an attractive target for cancer therapies not only for its prominent role in a number of malignancies but also for its scant expression in normal adult tissue. Therapeutic strategies that target ALK may provide ways to further delay...
TL13-112 is a PROTAC Degrader of ALK
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase and its mutation in domains. ALK Chromosomal translocations involve the kinase domain of ALK in many cancers. In addition to ALCL, ALK fusion proteins are seen in diffuse large B-cell lymphoma (DLBCL), inflammatory myofibroblastic tumor (IMT), breast cancer, colorectal cancer,...
MS4077 is an Anaplastic Lymphoma Kinase PROTAC (Degrader)
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase, which belongs to the insulin receptor kinase subfamily. ALK correlates with oncogenesis in different types of cancers, such as anaplastic large-cell non-Hodgkin’s lymphoma (ALCL), non-small-cell lung cancer (NSCLC), squamous cell carcinoma (SCC), renal cell carcinoma (RCC), thyroid cancer, breast cancer,...