Trk Receptor

ONO-7579 is an orally active TRKA inhibitor that suppresses tumor growth by inhibiting the phosphorylation of TRKA. In colorectal cancer cells KM12, its EC50 is 17.6 ng/g (meaning that when each gram of tumor tissue contains 17.6 ng of ONO-7579, the activity of phosphorylated TRKA in the tumor is inhibited by 50%). ONO-7579 can be used in cancer research.

Repotrectinib (Standard) is the analytical standard of Repotrectinib (HY-103022). This product is intended for research and analytical applications. 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.

Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [³⁵S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.

TrkA-IN-8 (Compound 2) is a TrkA inhibitor with a K_d value of 3.3 µM. RTKs-IN-1 exhibits concentration-dependent inhibition of cell proliferation in lung cancer cell lines. RTKs-IN-1 holds potential for research in non-small cell lung cancer .

Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. 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).

GNF-8625 is a broad-spectrum TRK inhibitor that can combine with Thalidomide to form a PROTAC degrader. The IC50 of GNF-8625 for inhibiting TRKA, TRKB, and TRKC are 0.8 nM, 22 nM, and 5.4 nM, respectively.

Eratrectinib (Example 1) is a Trk inhibitor. Eratrectinib can be studied in research for tropomyosin receptor kinase-related diseases and cancers.

AZD6918 is an orally active and selective Trk tyrosine kinase inhibitor. AZD6918 induces cell death as a single agent and attenuates BDNF/TrkB-induced protection from Etoposide (HY-13629) in vitro. AZD6918 can be used for the research of neuroblastoma.

HS-345 is a TrkA/Ak inhibitor with significant anti-pancreatic cancer effects. HS-345 inhibits the growth and proliferation of pancreatic cancer cells by targeting the TrkA/Akt signaling pathway, while also inducing apoptosis. Additionally, HS-345 suppresses blood vessel formation by decreasing the expression of HIF-1α and VEGF. HS-345 holds promise for research in pancreatic cancer.

CH7057288 (Standard) is the analytical standard of CH7057288 (HY-107362). This product is intended for research and analytical applications. CH7057288 is a potent and selective TRK inhibitor. CH7057288 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Udonitrectag (Standard) is the analytical standard of Udonitrectag (HY-109194). This product is intended for research and analytical applications. Udonitrectag (REC 0559), a low molecular weight compound that mimics NGF, aims to address the issue of NGF stability.

ANA-12 (Standard) is an analytical standard of ANA-12 (HY-12479). This product is intended for research and analytical applications. ANA-12 is a brain-penetrant, selective TrkB antagonist with IC₅₀ values of 45.6 nM and 41.1 μM, and K_d values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory.

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.

Larotrectinib sulfate (Standard) is the analytical standard of Larotrectinib sulfate. This product is intended for research and analytical applications. 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).

Selitrectinib (Standard) is the analytical standard of Selitrectinib. This product is intended for research and analytical applications. 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.

7,8-Dihydroxyflavone is a potent and selective TrkB agonist that mimics the physiological actions of Brain-derived neurotrophic factor (BDNF). Displays therapeutic efficacy toward various neurological diseases.

GBR-900 is a humanized antibody expressed in CHO that targets TrkA/NTRK1. GBR-900 has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for GBR-900 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

AZD-2066 hydrochloride is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrochloride activates the BDNF/trkB signaling pathway. AZD 2066 hydrochloride can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.

BNN-20 is a synthetic microneurotrophin that mimics brain-derived neurotrophic factor (BDNF) and exhibits area-specific pleiotropic neuroprotective and pro-neurogenic effects. BNN-20 can be utilized in research related to Parkinson's disease.

LM22B-10 (Standard) is the analytical standard of LM22B-10 (HY-104047). This product is intended for research and analytical applications. LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.