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Home > Inhibitors & Agonists > Tyrosine Kinase > Trk Receptor

Trk Receptor

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Cat. No. Product Name Field of Application Chemical Structure
DC10631 PF-06273340 Featured
PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.
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DC74435 PTX-BD10-2
PTX-BD10-2 (BD10-2) is a selective, brain-penetrant small molecule TrkB/C receptor partial agonist, shows survival-promoting activity.
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DC74434 Emzeltrectinib
Emzeltrectinib is a potent, selective neurotrophic factor tyrosine kinase receptor TrkB inhibitor, shows potential for treatment of Trk kinase-mediated tumor.
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DC74433 Anizatrectinib
Anizatrectinib is a potent and orally active inhibitor of TrkA kinase with potential for inflammatory disease such as prostatitis.
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DC8029 ANA-12 Featured
ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice.
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DC9837 Larotrectinib (LOXO-101 sulfate) Featured
LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
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DC8300 Entrectinib (RXDX-101) Featured
Entrectinib (RXDX-101), a potent and selective small molecule inhibitor of TrkA/B/C, ROS1, and ALK kinases, has demonstrated early clinical activity when orally administered intermittently under fasting conditions.
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DC10448 Belizatinib(TSR-011) Featured
Belizatinib(TSR-011) is an orally available inhibitor of both the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and the tropomyosin-related kinases (TRK) TRKA, TRKB, and TRKC, with potential antineoplastic activity.
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DC71253 IHMT-TRK-284
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies.
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DC71183 TIY-7
TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKAG595R, TRKAG667C, TRKAF589L, TRKCG623R, TRKCG696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model.
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DC71141 D5261
D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.
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DC70879 Utatrectinib
Utatrectinib (AZD7451, AZ12607092) is a potent, selective, small molecule pan-Trk (NTRK) inhibitor with IC50 of 0.2-3.0 nM against TrkA, TrkB, and TrkC.Binding of AZD7451 to TrkA, TrkB, and TrkC would be expected to inhibit responses associated with NGF, BDNF, and NT3, respectively.AZD7451 completely blocked TrkC activation and associated tumorigenic behaviors at sub-micromolar concentrations in normal salivary gland tissue.AZD7451 showed efficacy and low toxicity in pre-clinical studies on adenoid cystic carcinoma (ACC) tumors engrafted in mice.AZD7451 potently inhibited in vitro growth and proliferation of the KM12 cell line harboring the NTRK1-fusion at 2 nM, AZD7451 inhibited proliferation of H460 cells at 5 nM, with TRKA phosphorylation inhibition.
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DC70670 ONO-7579
ONO-7579 (ONO7579) is a novel potent, selective, orally available pan-TRK inhibitor.BDNF significantly increased TRKB phosphorylation in GBC cells and the effects were abrogated by ONO-7579, suppress proliferation in a dose-dependent manner in TYGBK-1 cells.ONO-7579 inhibited BDNF/TRKB-induced migration and invasiveness, particularly in GBC cells harboring wild-type KRAS.ONO-7579 reduced invasiveness of gallbladder cancer (GBC) cells through inhibiting epithelial–mesenchymal transition (EMT) via the extracellular signal-regulated kinase (ERK) or protein kinase B (AKT) pathway.
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DC70488 HJ-01
HJ-01 is a small molecule that disrupts PTPσ-Trk interaction, enhances Trk signaling, and promotes sympathetic nerve regeneration over chondroitin sulfate proteoglycans (CSPGs).
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DC70232 AZD 1332
AZD1332 is a potent, selective, ATP-competitive neurotrophic tyrosine kinase receptor (NRTK;TRK) inhibitor with IC50 of <10 nM; inhibits phosphorylation of TrkA/B/C in MCF10A cells overexpressing TrkA and NIH3T3 cells over expressing TrkA, TrkB, or TrkC with IC50 of <5 nM, inhibits a panel Baf3 survival driven by TrkA, TrkB, or TrkC with EC50 of 2 nM, AZD 1332 is orally available.
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DC50128 TRK-IN-12
TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRKG595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control drug LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line.
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DC50127 Trk-IN-9
Trk-IN-9 (Compound 12) is a potent inhibitor of TRK. Trk-IN-9 inhibits the proliferation of Km-12 cell lines. Trk-IN-9 induces the apoptosis of Km-12 cells in a concentration-dependent manner. Trk-IN-9 inhibits the phosphorylation of TRK to block downstream pathways. Trk-IN-9 has the potential for the research of NTRK-fusion cancers.
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DC50126 Trk-IN-11
Trk-IN-11 (Compound 14h) is a potent inhibitor of TRK (IC50 = 1.4, 1.8 nM, against TrkA, TrkAG595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key drug target in solid tumors. Trk-IN-11 has the potential for the research of cancer disease.
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DC50125 Trk-IN-10
Trk-IN-10 (Compound 14j) is a potent inhibitor of TRK (IC50 = 0.86, 6.92 nM, against TrkA, TrkAG595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key drug target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) has a higher selectivity of Trk inhibition, which may be of great significance for reducing toxicity.
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DC50124 Trk-IN-1
Trk-IN-1 (example 9), a potent tropomyosin-related kinase (Trk) inhibitor, shows potency against TrkA (3.7 nM) and TrkB (94 nM), respectively.
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DC50123 Trk-IN-8
Trk-IN-8 is a potent TRK inhibitor with IC50s of 0.42, 0.89 and 1.5 nM for TRKAa, TRKA(G595R) and TRKC(G623R), respectively (WO2021115401A1, compound 3).
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DC50122 Trk-IN-7
Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC50s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC50<15 nM) ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50=5-50 nM).
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DC7145 GW441756 Featured
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.
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DC11448 LOXO 195(Selitrectinib) Featured
LOXO-195 is a next-generation TRK kinase (TKI) inhibitor, with IC50s of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC respectively.
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DC47324 Trk-IN-6
Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).
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DC46609 Cyclotraxin B TFA
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50  of  0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
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DC45818 LPM4870108
LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity.
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DC45284 Cyclotraxin B
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50  of  0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
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DC41628 BDNF(human)
BDNF (human) is a neurotrophin in the central nervous system?and mediates survival and differentiation of neurons. BDNF (human) binds to TrkB and leads to the dimerization and autophosphorylation of tyrosine residues in the intracellular domain of the receptor. BDNF (human) can be used for study of neurodegenerative and psychiatric disorder.
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DC40576 GNF-8625 monopyridin-N-piperazine hydrochloride
GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1.
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