Trk Receptor Inhibitor

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.

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.

BBT-176 is an orally active EGFR tyrosine kinase inhibitor. BBT-176 is a reversible ATP-competitive inhibitor with a unique binding mode, and it exhibits selectivity for mutant EGFR over wild-type EGFR. BBT-176 inhibits tumor growth, induces tumor regression, upregulates EGFR expression, and does not trigger secondary EGFR gene mutations. BBT-176 can be used in research related to non-small cell lung cancer.

Trk-IN-2 is an orally active pan-Trk kinase inhibitor with an TrkA IC₅₀ of 9 nM. Trk-IN-2 exhibits pharmacodynamic effects in rat models of inflammatory pain and neuropathic pain.Trk-IN-2 can be used for the research of inflammatory pain, neuropathic pain.

Izenivetmab (ZTS-00075623) is an anti-NGFB IgG2κ monoclonal antibody. Izenivetmab shows anti-inflammatory and analgesic effects by targeting anti-nerve growth factor (NGF). Izenivetmab can be used for the research of osteoarthritis.

Fasinumab (Anti-Human NGF) is a human IgG4 monoclonal antibody to nerve growth factor (NGF). Fasinumab can be used in acute sciatica and knee osteoarthritis (OA) studies.

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 K_i 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.

Fulranumab is a human IgG2 monoclonal antibody against nerve growth factor (NGF) and can be used for the research of pain.

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice.

Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.

2-Bromo-6-methoxynaphthalene is an active intermediate in the production of anti-inflammatory agents like Naproxen and Nabumetone by Heck reaction. 2-Bromo-6-methoxynaphthalene has potential anti-inflammatory properties and Tyrosine-protein inhibitor properties. 2-Bromo-6-methoxynaphthalene can be used for the research of cancer.

Pz-1 is a potent RET and VEGFR2 inhibitor with IC₅₀s of less than 1 nM for both wild type kinases.

ALK-IN-28 (compound 22) is an inhibitor of anaplastic lymphoma kinase (ALK).

Ganglioside GM1-binding peptide p3 is a synthetic peptide that can specifically bind to the pentasaccharide part of GM1 ganglioside. The dynamic transformation of Ganglioside GM1-binding peptide p3 may play an important role in the function of GM1 as a multiple receptor, such as in the classical pathway of cholera toxin infection. Ganglioside GM1-binding peptide p3 can be used to study the interaction between GM1 and its ligands.

c-Fms-IN-3 is an orally active c-Fms (CSF1R) kinase inhibitor (IC₅₀ = 0. 8 nM). c-Fms-IN-3 inhibits CSF1R kinase activity and reduces macrophage populations. c-Fms-IN-3 reduces bone erosion, pannus invasion, cartilage damage, and inflammation in collagen (HY-NP003)-induced arthritis mouse model. c-Fms-IN-3 is useful for arthritis research.

Povovetug is a humanized IgG1κ chimeric monoclonal antibody inhibitor targeting NGF/bNGF. Povovetug has a significant analgesic activity. Povovetug can be used for central neuroinflammation like chronic radicular pain research.

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.

Luvagrobart is an anti-NGF human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 (PLK4) (IC₅₀=2.6 nM). CZS-241 hydrochloride inhibits TRKA with an IC₅₀ value of 2.74 μM. CZS-241 hydrochloride induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 hydrochloride shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.