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TrkA Inhibitor

" in MedChemExpress (MCE) Product Catalog:

125

Inhibitors & Agonists

3

Peptides

4

Inhibitory Antibodies

1

Natural
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3

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12678
    Entrectinib
    Maximum Cited Publications
    28 Publications Verification

    NMS-E628; RXDX-101

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib
  • HY-12866
    Larotrectinib
    15+ Cited Publications

    LOXO-101; ARRY-470

    Trk Receptor Apoptosis Cancer
    Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
    Larotrectinib
  • HY-103022
    Repotrectinib
    5+ Cited Publications

    TPX-0005

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Cancer
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity .
    Repotrectinib
  • HY-14721
    Tepotinib
    5+ Cited Publications

    EMD-1214063

    c-Met/HGFR Autophagy Cancer
    Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects .
    Tepotinib
  • HY-13491
    GNF-5837
    4 Publications Verification

    Trk Receptor Cancer
    GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
    GNF-5837
  • HY-50867
    Lestaurtinib
    4 Publications Verification

    CEP-701; KT-5555

    JAK FLT3 Trk Receptor Apoptosis STAT Cancer
    Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor .
    Lestaurtinib
  • HY-108466
    Ro 08-2750
    4 Publications Verification

    Apoptosis Neurological Disease Cancer
    Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 μM. Ro 08-2750 inhibits NGF binding to p75 NTR selectively over TRKA . Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM .
    Ro 08-2750
  • HY-10200
    BMS-754807
    10+ Cited Publications

    IGF-1R Insulin Receptor Endocrinology Cancer
    BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively .
    BMS-754807
  • HY-101977
    Selitrectinib
    5 Publications Verification

    LOXO-195

    Trk Receptor Cancer
    Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively .
    Selitrectinib
  • HY-18314
    GW 441756
    5+ Cited Publications

    Trk Receptor Apoptosis Neurological Disease Cancer
    GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC50=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth .
    GW 441756
  • HY-P99297

    ZTS-00508841

    Trk Receptor Inflammation/Immunology
    Bedinvetmab (ZTS-00508841) is a canine monoclonal antibody (mAb) targeting nerve growth factor (NGF). Bedinvetmab inhibits NGF interaction with tropomyosin receptor kinase A (trkA) and p75 neurotrophin receptor (p75NTR) receptors. Bedinvetmab can be used for the research of osteoarthritis pain in dogs .
    Bedinvetmab
  • HY-10424
    Milciclib
    5+ Cited Publications

    PHA-848125

    CDK Autophagy Cancer
    Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
    Milciclib
  • HY-148811

    ICP-723

    c-Met/HGFR Trk Receptor Cancer
    Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC50 = 0.81 nM; TRKB IC50 = 0.145 nM; TRKC IC50 = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma .
    Zurletrectinib
  • HY-12866A
    Larotrectinib sulfate
    15+ Cited Publications

    LOXO-101 sulfate; ARRY-470 sulfate

    Trk Receptor Apoptosis Cancer
    Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
    Larotrectinib sulfate
  • HY-137465

    PROTACs Trk Receptor Cancer
    CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma .
    CG428
  • HY-15590
    AZ-23
    3 Publications Verification

    AZD1332

    Trk Receptor Cancer
    AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
    AZ-23
  • HY-122616

    Trk Receptor Neurological Disease
    PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain .
    PF-06273340
  • HY-17603
    Belizatinib
    1 Publications Verification

    TSR-011

    Anaplastic lymphoma kinase (ALK) Trk Receptor Cancer
    Belizatinib (TSR-011) is an orally active, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
    Belizatinib
  • HY-20878
    Tyrphostin AG 879
    3 Publications Verification

    AG 879

    Trk Receptor EGFR Apoptosis Cancer
    Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity .
    Tyrphostin AG 879
  • HY-114331

    MAP3K FLT3 PAK STK33 Trk Receptor Neurological Disease
    DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a Ki value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research .
    DLK-IN-1
  • HY-129634

    Trk Receptor Neurological Disease
    TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity .
    TrkA-IN-1
  • HY-145587

    PBI-200; PPI-5278

    Tyrosinase Trk Receptor Inflammation/Immunology Cancer
    Paltimatrectinib (compound I-147) is a potent tyrosine kinase inhibitor with an IC50 of <10 nM for tropomyosin kinases A (TrkA). Paltimatrectinib has the potential for cancer and inflammatory diseases .
    Paltimatrectinib
  • HY-112436

    Trk-IN-4

    Trk Receptor Neurological Disease
    PF-6683324 (Trk-IN-4) is a potent pan-Trk inhibitor in cell-based assays with IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
    PF-6683324
  • HY-114357A

    TAM Receptor c-Met/HGFR Trk Receptor Cancer
    DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo .
    DS-1205b free base
  • HY-14721R

    EMD-1214063 (Standard)

    Reference Standards c-Met/HGFR Autophagy Cancer
    Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects .
    Tepotinib (Standard)
  • HY-149912

    Polo-like Kinase (PLK) Trk Receptor Apoptosis Cancer
    CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines .
    CZS-241
  • HY-151948

    Trk Receptor Neurological Disease
    TrkA-IN-3 is a potent, subselective and allosteric TrkA inhibitor, with an IC50 of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC. TrkA-IN-3 can be used for the research of pain .
    TrkA-IN-3
  • HY-151949

    Trk Receptor Neurological Disease
    TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC50=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects .
    TrkA-IN-4
  • HY-157542

    Trk Receptor PROTACs Others
    CG428-NEG is a TRK degrader negative control. CG428 (HY-137465) inhibits cell growth and reduce TPM3-TRKA levels .
    CG428-NEG
  • HY-112471

    CDK Cancer
    TrkA Inhibitor (Compound 18) is a CDK2 inhibitor with an IC50 of 0.69  μM over CDK1. TrkA Inhibitor can be used for chemotherapy-induced alopecia research .
    TrkA Inhibitor
  • HY-122906

    c-Fms Inflammation/Immunology
    JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis .
    JTE-952
  • HY-112437

    Trk Receptor Neurological Disease
    PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
    PF-06737007
  • HY-14721A

    EMD-1214063 hydrochloride

    c-Met/HGFR Autophagy Cancer
    Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects .
    Tepotinib hydrochloride
  • HY-135096

    Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease
    Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
    Amitriptyline-d3 hydrochloride
  • HY-171450

    Trk Receptor Cancer
    VMD-928 is an orally active, allosteric, irreversible and selective tropomyosin receptor kinase A (TrkA) inhibitor. VMD-928 blocks the downstream signaling pathways triggered by the binding of nerve growth factor (NGF) to TrkA, thereby inhibiting cell proliferation, invasion, and promoting cancer cell death. VMD-928 is promising for research of various cancers, including prostate cancer, thymic carcinoma, mesothelioma, squamous cell carcinoma of the head and neck, squamous cell carcinoma of the lung, ovarian cancer, hepatocellular carcinoma .
    VMD-928
  • HY-P3709

    p62 E1/E2/E3 Enzyme Neurological Disease
    TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke .
    TRAF6 peptide
  • HY-141864

    Itk Inflammation/Immunology
    ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
    ITK/TRKA-IN-1
  • HY-P991622

    Trk Receptor Neurological Disease Inflammation/Immunology
    MNAC13 is a kind of mouse IgG1 chimeric antibody, targeting to human TrkA. MNAC13 inhibits the NGF dependent signaling pathway by specifically binding to TrkA receptors. MNAC13 has good analgesic effect and long-lasting efficacy. MNAC13 can be used for researches on inflammatory and chronic pain .
    MNAC13
  • HY-131244

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively .
    ALK-IN-9
  • HY-112423

    Trk Receptor Tie Cardiovascular Disease Cancer
    CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
    CE-245677
  • HY-175271

    PROTACs Trk Receptor ERK Cancer
    JWJ-01-378 is a selective TRK PROTAC degrader. JWJ-01-378 efficiently degrades WT TRK and TPM3-TRKA fusion proteins and inhibits downstream pERK signaling, while showing limited efficacy against TRK inhibitor resistant mutants and ALK fusions. JWJ-01-378 potently suppresses cancer cell proliferation .Pink: TRK ligand (HY-160520); Blue: CRBN ligase ligand (HY-103596); Black: linker
    JWJ-01-378
  • HY-146697

    Trk Receptor c-Fms PDGFR Bcr-Abl c-Kit Apoptosis Cancer
    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 .
    IHMT-TRK-284
  • HY-P3709A

    p62 E1/E2/E3 Enzyme Neurological Disease
    TRAF6 peptide TFA is a specific TRAF6-p62 inhibitor. TRAF6 peptide TFA potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide TFA has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke .
    TRAF6 peptide TFA
  • HY-124637

    Trk Receptor Neurological Disease
    ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC50 values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the study of pain .
    ALE-0540
  • HY-157168

    Trk Receptor Neurological Disease
    TrkA-IN-6 (compound R48) is a hydrazone-like, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). TrkA-IN-6 exhibited a higher cytotoxic effect on U87 GBM cells than Temozolomide (HY-17364), with an IC50 of 68.99 μM .
    TrkA-IN-6
  • HY-178142

    EGFR VEGFR Trk Receptor CDK FAK Akt GSK-3 Apoptosis Caspase Bcl-2 Family Cancer
    Multi-kinase-IN-7 is a multikinase inhibitor with IC50s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC50 values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer .
    Multi-kinase-IN-7
  • HY-172802

    Trk Receptor Cancer
    TrkA-IN-10 (PI-15R) is a TrkA inhibitor with the IC50 values of 17 nM, 8 nM, and 5 nM for TrkA, TrkB and TrkC, respectively. TrkA-IN-10 can be used in cancer research .
    TrkA-IN-10
  • HY-169546

    Trk Receptor Cancer
    TrkA-IN-7 (Compound 4) is an inhibitor of Tropomyosin Receptor Kinase A (TrkA) with a Kd value of 40 μM .
    TrkA-IN-7
  • HY-161775

    RET Trk Receptor Cancer
    RET/TRKA-IN-1 (Compound 13) is a dual inhibitor for RET (IC50=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits cell viability of LC-2 and KM12, with GI50 of 0.72 and 0.25 μM. RET/TRKA-IN-1 arrests the cell cycle at G1 phase .
    RET/TRKA-IN-1
  • HY-161819

    Trk Receptor Cancer
    TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA G595R, TRKA F589L, TRKA G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .
    TRK-IN-29

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