trk

Trk-IN-9 (Compound 12) is a potent inhibitor of TRK that inhibits the proliferation of Km-12 cell lines and induces apoptosis in a concentration-dependent manner. It also inhibits TRK phosphorylation and blocks downstream pathways, showing potential for NTRK fusion cancer research.

GNF-8625 monopyridin-N-piperazine hydrochloride is a tropomyosin receptor kinase (TRK) inhibitor.

CG 428 is a potent tropomyosin receptor Kinase (TRK) Degrader (uSMITETM) with a DC50 of 0.36 nM. CG 428 comprises an analog of the pan-TRK inhibitor GNF-8625 joined by a linker to the cereblon E3 ligase ligand pomalidomide. CG 428 shows selectivity for TRKA over TRKC and TRKB with Kds of 1nM, 4.2 nM, and 28 nM. CG 428 inhibits the growth of KM12 colon cancer cells with an IC50 of 2.9 nM.

Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Thalidomide-5-NH2-CH2-COOH (compound 114) is a selective inhibitor of the protomyosin receptor kinase and a ligand for E3 ligase, offering potential for studying various diseases.

CH7057288 is an effective and selective TRK inhibitor with an IC50 value of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB and TRKC, respectively.

Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).

Tyrphostin AG 879 (AG 879) effectively inhibits HER2/ErbB2 with an IC50 of 1 μM, demonstrating 100- and 500-fold higher selectivity for ErbB2 over EGFR and PDGFR, respectively.

Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively).

LM22A-4 is a brain-derived neurotrophic factor (BDNF) mimetic and agonist of the receptor tropomyosin-related kinase B (TrkB; IC50 : 47 nM in a fluorescence anisotropy assay)

(6RS)-LOXO-195 (BAY 2731954) is a potent and selective Trk tyrosine kinase inhibitor.

DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family.

Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA/TrkB/TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5 nM for TRKA, 0.7 nM for TRKB, and 2.6 nM for TRKC. The compound demonstrates good selectivity within the kinase group and exhibits significant anti-tumor efficacy in vivo.

TRK-IN-30 (Compound C11) is an inhibitor of tropomyosin receptor kinases (TRK), effectively inhibiting TRKA, TRKB, TRKC, and the resistant mutant TRKAG595R, with IC50 values of 1.8, 0.98, 3.8, and 54 nM, respectively. It also suppresses the activation of downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 hinders colony formation and cell migration of Km-12, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis in Km-12 cells.

Type II TRK inhibitor 2 (compound 40l) is a selective Type II TRK inhibitor characterized by plasma stability and moderate liver microsome stability. It significantly impedes the proliferation of Km-12, Ba/F3-TRKAG595R, and Ba/F3-TRKAG667C cells with IC50 values of 4.1 nM, 41.5 nM, and 1.4 nM, respectively. Type II TRK inhibitor 2 is applicable for research into NTRK fusion cancers.

TRK-IN-27 (Compound 14q) is a potent inhibitor of TRK with excellent kinase selectivity, effectively suppressing tumor growth.

TRK-IN-22 (compound 11) is an inhibitor of TRK. This compound functions as a classic type I inhibitor, effectively occupying the ATP binding pocket of TRKA.

TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor with IC50 values of 9 nM for TRKAG595R, 0.6 nM for TRKAF589L, 18 nM for TRKAG667C, 5 nM for TRKA, and 6 nM for TRKC. It effectively inhibits the phosphorylation of TRKA and demonstrates significant antiproliferative activity against NTRK fusion-positive cells. TRK-IN-29 also exhibits excellent plasma stability and moderate pharmacokinetic properties.

DDR-TRK-1N is a negative control for DDR-TRK-1.

TRK-380 (TAC-301) is an effective and selective β3-adrenergic receptor agonist. TRK-380 improves formalin-induced frequent urination in rats and carbachol-induced bladder contraction in dogs (a decrease of 37.6%).

TRK-IN-15 (WO2012034091A1, compound X-55) is a highly effective inhibitor of TRK, a protein kinase with crucial involvement in the regulation of cellular growth, differentiation, and signal transduction. Offering significant potential for studying TRK-related diseases, TRK-IN-15 holds promise for advancing research in this field [1].

TRK-IN-16 (WO2012034091A1, compound X-21) is a highly effective TRK inhibitor, targeting protein kinases that are integral to regulating cell growth, differentiation, and various cellular signal transduction processes. This compound shows great potential for research in TRK-related diseases [1].

Trk-IN-7 (compound I-6) is a highly potent TRK inhibitor, with IC50 values of 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. It also shows significant inhibition of EML4-ALK (IC50 <15 nM) and ALK mutations G1202R, C1156Y, R1275Q, F1174L, L1197M, and G1269A (IC50 = 5-50 nM) [1].