Preferred Label : ROS1/NTRK Inhibitor ANS03;
NCIt synonyms : NTRK/ROS1 Inhibitor ANS03;
NCIt definition : An orally bioavailable type II inhibitor of the receptor tyrosine kinase c-ros oncogene
1 (ROS1) and the neurotrophic tyrosine receptor kinases (NTRKs), with potential antineoplastic
activity. Upon oral administration, ROS1/NTRK inhibitor ANS03 selectively targets
and specifically binds to the inactive DFG-out conformations of ROS1 and NTRK, including
various pathogenetic ROS1/NTRK alterations such as ROS1 G2032R, D2033N, L2086F and
NTRK G667C, G595R, G667C, and inhibits their activity. This inhibition leads to a
disruption of ROS1- and NTRK-mediated signaling and eventually inhibits the growth
of tumor cells that are overexpressing ROS1 and/or NTRKs. ROS1, overexpressed in certain
cancer cells, plays a key role in cell growth and survival of cancer cells. NTRK mutations
or rearrangements play a key role in cancer progression. ANS03 may overcome on-target
acquired resistance mutations.;
Molecule name : ANS 03; ANS-03;
Origin ID : C217362;
concept_is_in_subset
- has_target
