type i trk inhibitor (az-23) (AstraZeneca ltd)
90
Structured Review
AstraZeneca ltd
type i trk inhibitor (az-23)
Type I Trk Inhibitor (Az 23), supplied by AstraZeneca ltd, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/az-23/az+23/pm39033612-31-9-2
Average 90 stars, based on 1 article reviews
Type I Trk Inhibitor (Az 23), supplied by AstraZeneca ltd, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/az-23/az+23/pm39033612-31-9-2
Average 90 stars, based on 1 article reviews
type i trk inhibitor (az-23) - by Bioz Stars,
2026-11
90/100 stars
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Inhibition:Article Title: Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance. Article Snippet: Tropomyosin receptor kinase (TRK) is a promising target for treating NTRK fusion cancers.. The solvent front and xDFG mutations induced by larotrectinib and entrectinib result in acquired resistance in advanced-stage patients.. In this study, we report a highly potent and selective type II TRK inhibitor, 40l, developed using a structure-based design strategy. Article Title: "On Trk " - the TrkB signal transduction pathway is an increasingly important target in cancer biology Article Snippet: Another series of Trk inhibitors came from the optimization of Article Title: Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo. Article Snippet: Herein, we report the discovery process and antitumor activity of the TRK inhibitor CZw-124 (8o), which is a quinazoline derivative.. Starting from a PAK4 inhibitor, we used various drug design strategies, including pharmacophore feature supplementation, F-scanning, and blocking metabolic sites, and finally found a TRK inhibitor CZw-124 that is effective in vitro and in vivo.. Docking studies and molecular dynamics simulations revealed a possible mode of binding of CZw-124 to TRKA. Article Title: K252a induces anoikis-sensitization with suppression of cellular migration in Epstein-Barr virus (EBV)--associated nasopharyngeal carcinoma cells. Article Snippet: Recent studies revealed an unexpected role of the neurotrophin receptor pathway, BDNF/TrkB signaling, in cancer metastasis and anoikis (i.e. detachment-induced cell death).. Survival of cancer cells in detached state (known as anoikis-resistance) is known to be pre-requisite for metastasis.. Nasopharyngeal carcinoma (NPC), an endemic head and neck cancer in Southeast Asia, is highly invasive, metastatic, and etiologically associated with Epstein-Barr virus (EBV, an oncovirus) infection. Article Title: On Trk—The TrkB Signal Transduction Pathway Is an Increasingly Important Target in Cancer Biology: Fig. 1. Article Snippet: In pediatrics, the New Agents in Neuroblastoma Therapy (NANT) consortium has an open trial N2001-03: “A Phase I study of CEP-701 in Patients with Refractory Neuroblastoma.”1 Another series of Trk inhibitors came from the optimization of Article Title: Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review. Article Snippet: The tropomyosin receptor tyrosine kinases (TRKs) control the cell proliferation mainly in the nervous system and are encoded by NTRK genes.. Fusion and mutation of NTRK genes were detected in various types of cancers.. Many small molecules TRK inhibitors have been discovered during the last two decades and some of them have entered clinical trials. Article Title: Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain. Article Snippet: The neurotrophin nerve growth factor (NGF) has been implicated as a key mediator of chronic pain.. NGF binds the tropomysin receptor kinase A (TrkA) and p75, resulting in the activation of downstream signaling pathways that have been linked to pro-nociception.. While anti-NGF antibodies have demonstrated analgesia both preclinically and in patients, the mechanism of action of these agents remains unclear. Article Title: Design, synthesis, and biological evaluation of aminopyridine derivatives as novel tropomyosin receptor kinase inhibitors. Article Snippet: Correspondence Dongmei Zhao, Key Laboratory of Structure‐ Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Rd, Shenhe District, Shenyang 110016, China.. Email: medchemzhao@163.com Abstract Tropomyosin receptor kinase (TRK) is a successful target for the treatment of various cancers caused by NTRK gene fusions.. Herein, based on a rational drug design strategy, we designed and synthesized 35 aminopyrimidine derivatives that were shown to be TRKA inhibitors in the enzyme assay, among which compounds C3, C4, and C6 showed potent inhibitory activities against TRKA with IC50 values of 6.5, 5.0, and 7.0 nM, respectively. In Vivo:Article Title: Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance. Article Snippet: Tropomyosin receptor kinase (TRK) is a promising target for treating NTRK fusion cancers.. The solvent front and xDFG mutations induced by larotrectinib and entrectinib result in acquired resistance in advanced-stage patients.. In this study, we report a highly potent and selective type II TRK inhibitor, 40l, developed using a structure-based design strategy. Article Title: "On Trk " - the TrkB signal transduction pathway is an increasingly important target in cancer biology Article Snippet: Another series of Trk inhibitors came from the optimization of Article Title: Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo. Article Snippet: Herein, we report the discovery process and antitumor activity of the TRK inhibitor CZw-124 (8o), which is a quinazoline derivative.. Starting from a PAK4 inhibitor, we used various drug design strategies, including pharmacophore feature supplementation, F-scanning, and blocking metabolic sites, and finally found a TRK inhibitor CZw-124 that is effective in vitro and in vivo.. Docking studies and molecular dynamics simulations revealed a possible mode of binding of CZw-124 to TRKA. Article Title: K252a induces anoikis-sensitization with suppression of cellular migration in Epstein-Barr virus (EBV)--associated nasopharyngeal carcinoma cells. Article Snippet: Recent studies revealed an unexpected role of the neurotrophin receptor pathway, BDNF/TrkB signaling, in cancer metastasis and anoikis (i.e. detachment-induced cell death).. Survival of cancer cells in detached state (known as anoikis-resistance) is known to be pre-requisite for metastasis.. Nasopharyngeal carcinoma (NPC), an endemic head and neck cancer in Southeast Asia, is highly invasive, metastatic, and etiologically associated with Epstein-Barr virus (EBV, an oncovirus) infection. Article Title: On Trk—The TrkB Signal Transduction Pathway Is an Increasingly Important Target in Cancer Biology: Fig. 1. Article Snippet: In pediatrics, the New Agents in Neuroblastoma Therapy (NANT) consortium has an open trial N2001-03: “A Phase I study of CEP-701 in Patients with Refractory Neuroblastoma.”1 Another series of Trk inhibitors came from the optimization of Article Title: Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review. Article Snippet: The tropomyosin receptor tyrosine kinases (TRKs) control the cell proliferation mainly in the nervous system and are encoded by NTRK genes.. Fusion and mutation of NTRK genes were detected in various types of cancers.. Many small molecules TRK inhibitors have been discovered during the last two decades and some of them have entered clinical trials. Article Title: Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain. Article Snippet: The neurotrophin nerve growth factor (NGF) has been implicated as a key mediator of chronic pain.. NGF binds the tropomysin receptor kinase A (TrkA) and p75, resulting in the activation of downstream signaling pathways that have been linked to pro-nociception.. While anti-NGF antibodies have demonstrated analgesia both preclinically and in patients, the mechanism of action of these agents remains unclear. Article Title: Design, synthesis, and biological evaluation of aminopyridine derivatives as novel tropomyosin receptor kinase inhibitors. Article Snippet: Correspondence Dongmei Zhao, Key Laboratory of Structure‐ Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Rd, Shenhe District, Shenyang 110016, China.. Email: medchemzhao@163.com Abstract Tropomyosin receptor kinase (TRK) is a successful target for the treatment of various cancers caused by NTRK gene fusions.. Herein, based on a rational drug design strategy, we designed and synthesized 35 aminopyrimidine derivatives that were shown to be TRKA inhibitors in the enzyme assay, among which compounds C3, C4, and C6 showed potent inhibitory activities against TRKA with IC50 values of 6.5, 5.0, and 7.0 nM, respectively. Activity Assay:Article Title: Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance. Article Snippet: Tropomyosin receptor kinase (TRK) is a promising target for treating NTRK fusion cancers.. The solvent front and xDFG mutations induced by larotrectinib and entrectinib result in acquired resistance in advanced-stage patients.. In this study, we report a highly potent and selective type II TRK inhibitor, 40l, developed using a structure-based design strategy. Article Title: "On Trk " - the TrkB signal transduction pathway is an increasingly important target in cancer biology Article Snippet: Another series of Trk inhibitors came from the optimization of Article Title: Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo. Article Snippet: Herein, we report the discovery process and antitumor activity of the TRK inhibitor CZw-124 (8o), which is a quinazoline derivative.. Starting from a PAK4 inhibitor, we used various drug design strategies, including pharmacophore feature supplementation, F-scanning, and blocking metabolic sites, and finally found a TRK inhibitor CZw-124 that is effective in vitro and in vivo.. Docking studies and molecular dynamics simulations revealed a possible mode of binding of CZw-124 to TRKA. Article Title: K252a induces anoikis-sensitization with suppression of cellular migration in Epstein-Barr virus (EBV)--associated nasopharyngeal carcinoma cells. Article Snippet: Recent studies revealed an unexpected role of the neurotrophin receptor pathway, BDNF/TrkB signaling, in cancer metastasis and anoikis (i.e. detachment-induced cell death).. Survival of cancer cells in detached state (known as anoikis-resistance) is known to be pre-requisite for metastasis.. Nasopharyngeal carcinoma (NPC), an endemic head and neck cancer in Southeast Asia, is highly invasive, metastatic, and etiologically associated with Epstein-Barr virus (EBV, an oncovirus) infection. Article Title: On Trk—The TrkB Signal Transduction Pathway Is an Increasingly Important Target in Cancer Biology: Fig. 1. Article Snippet: In pediatrics, the New Agents in Neuroblastoma Therapy (NANT) consortium has an open trial N2001-03: “A Phase I study of CEP-701 in Patients with Refractory Neuroblastoma.”1 Another series of Trk inhibitors came from the optimization of Article Title: Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review. Article Snippet: The tropomyosin receptor tyrosine kinases (TRKs) control the cell proliferation mainly in the nervous system and are encoded by NTRK genes.. Fusion and mutation of NTRK genes were detected in various types of cancers.. Many small molecules TRK inhibitors have been discovered during the last two decades and some of them have entered clinical trials. Article Title: Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain. Article Snippet: The neurotrophin nerve growth factor (NGF) has been implicated as a key mediator of chronic pain.. NGF binds the tropomysin receptor kinase A (TrkA) and p75, resulting in the activation of downstream signaling pathways that have been linked to pro-nociception.. While anti-NGF antibodies have demonstrated analgesia both preclinically and in patients, the mechanism of action of these agents remains unclear. Article Title: Design, synthesis, and biological evaluation of aminopyridine derivatives as novel tropomyosin receptor kinase inhibitors. Article Snippet: Correspondence Dongmei Zhao, Key Laboratory of Structure‐ Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Rd, Shenhe District, Shenyang 110016, China.. Email: medchemzhao@163.com Abstract Tropomyosin receptor kinase (TRK) is a successful target for the treatment of various cancers caused by NTRK gene fusions.. Herein, based on a rational drug design strategy, we designed and synthesized 35 aminopyrimidine derivatives that were shown to be TRKA inhibitors in the enzyme assay, among which compounds C3, C4, and C6 showed potent inhibitory activities against TRKA with IC50 values of 6.5, 5.0, and 7.0 nM, respectively. |