Trk receptors are a family of three receptor tyrosine kinases (TrkA, TrkB, and TrkC), each of which can be activated by one or more of the four neurotrophins nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), and neurotrophins 3 and 4 (NT3 and NT4).
The TRK receptor family is made up of the transmembrane proteins TrkA, TrkB, and TrkC. These receptor tyrosine kinases are expressed in human neuronal tissue and are crucial for the physiology of nervous system development and function. Neurotrophins (NTs) activate these receptor tyrosine kinases. For TrkA, BDGF, NT-4/5, and TrkB and TrkC, respectively, these latter substances are specific ligands known as NGF and NT-3.
When a ligand binds to a receptor, the receptors begin to oligomerize and certain tyrosine residues in the intracytoplasmic kinase domain become phosphorylated. As a result of this action, signal transduction pathways that promote proliferation, differentiation, and survival in both healthy and malignant neuronal cells are activated.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V104559 | TRK-IN-30 | TRK-IN-30 (compound C11) is an inhibitor of tropomyosin receptor kinase (TRK), which can inhibit TRKA, TRKB, TRKC and the drug-resistant mutant TRKAG595R with IC50 of 1.8, 0.98, 3.8 and 54 nM, respectively. | |
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V69596 | Trk-IN-6 | 2489327-43-5 | Trk-IN-6 has excellent potency against TRK mutants in vitro (IC50 = 0.2-0.7 nM). |
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V69603 | Trk-IN-7 | 2383011-61-6 | Trk-IN-7 (compound I-6) is a potent Trk inhibitor (antagonist) with IC50 of 0.25-10 nM for TRKA, TRKB and TRKC respectively. |
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V69591 | Trk-IN-8 | 2762200-57-5 | Trk-IN-8 is a potent TRKA inhibitor (antagonist) with IC50 of 0.42, 0.89 and 1.5 nM for TRKAa, TRKA(G595R) and TRKC(G623R) respectively (WO2021115401A1, compound 3). |
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V69584 | TrkA-IN-1 | 1680179-43-4 | TrkA-IN-1 is a potent and specific inhibitor of myosin-related kinase A (TrkA) with IC50 of 99 nM in a cell-based assay. |
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V76395 | TrkA-IN-3 | 3026111-73-6 | TrkA-IN-3 is a potent and subselective allosteric inhibitor of TrkA with IC50 of 22.4 nM. |
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V76394 | TrkA-IN-4 | 3026111-74-7 | TrkA-IN-4 is a potent and orally bioactive allosteric inhibitor of TrkA and the precursor of TrkA-IN-3. |
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V81624 | TrkA-IN-6 | TrkA-IN-6 (compound R48) is a hydrazone, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). | |
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V69598 | TrkB-IN-1 | 1609067-49-3 | TrkB-IN-1 is a potent orally bioactive TrkB agonist/activator with good pharmacokinetic properties. |
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V69593 | Type II TRK inhibitor 1 | 2937543-72-9 | Type II TRK?inhibitor 1 is a potent TRK inhibitor that can suppress various TRK fusion protein variants and wild type. |
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V78315 | Type II TRK inhibitor 2 | Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor (antagonist) with plasma stability and moderate hepatic microsomal stability. | |
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V2683 | Larotrectinib (LOXO-101; ARRY-470) | 1223403-58-4 | Larotrectinib (LOXO-101; LOXO101; ARRY470;ARRY-470; Vitrakvi)is an orally bioactive, highly selective, ATP competitive TRK inhibitor with potential anticancer activity. |
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V2599 | Larotrectinib sulfate (LOXO-101; ARRY-470) | 1223405-08-0 | Larotrectinib sulfate (LOXO-101; ARRY-470; Vitrakvi), the suldate salt of Larotrectinib,is a potent, oral, selective, ATP competitive TRK inhibitor with IC50s in low nanomolar range (2 to 20 nM) for inhibition of all TRK family members in binding and cellular assays. |
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V2684 | Selitrectinib (BAY 2731954; LOXO-195) | 2097002-61-2 | Selitrectinib (also known as BAY-2731954;LOXO-195) is a 2nd generation, potent and selective TRK TKI (tyrosine kinase inhibitor) designed to overcome acquired resistance mediated by recurrent kinase domain (solvent front and xDFG) mutations identified in multiple patients who have developed resistance to other TRK TKIs such aslarotrectinib (LOXO-101). |
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