GNF-5837 (GNF5837) is an orally bioavailable pan-TRK (TrkA, TrkB) inhibitor with potential antitumor activity.
Larotrectinib sulfate (LOXO-101; ARRY-470; Vitrakvi), the suldate salt of Larotrectinib, is a potent, oral, selective, ATP competitive TRK inhibitor with IC50s in low nanomolar range (2 to 20 nM) for inhibition of all TRK family members in binding and cellular assays.
ANA-12 (ANA12) is a novel, potent and selective TrkB inhibitor/antagonist with important biological activity.
Larotrectinib (LOXO-101; LOXO101; ARRY470; ARRY-470; Vitrakvi) is an orally bioactive, highly selective, ATP competitive TRK inhibitor with potential anticancer activity.
PF-06273340 is a potent, selective, and well-tolerated pan-Trk inhibitor with IC50 of 6, 4, 3 nM for TrkA, TrkB, Trk C respectively.
LM22B-10 (LM22B10) is a novel, potent activator of TrkB/TrkC (Tropomyosin-receptor kinase) neurotrophin receptor, inducing TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
CH7057288 is a novel, potent and selective inhibitor of TRK (tyrosine receptor kinase) with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.
Selitrectinib (also known as BAY-2731954; LOXO-195) is a 2nd generation, potent and selective TRK TKI (tyrosine kinase inhibitor) designed to overcome acquired resistance mediated by recurrent kinase domain (solvent front and xDFG) mutations identified in multiple patients who have developed resistance to other TRK TKIs such as larotrectinib (LOXO-101).
GW441756 (GW-441756) is a novel, potent and selective inhibitor of TrkA (Tropomyosin-related kinase A) with potential anticancer activity.