trk

DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family.

Trk-IN-4 is an effective pan-Trk inhibitor in cell-based assays (IC50s: 1.9 nM, 2.6 nM, and 1.1 nM for TrkA, TrkB, and TrkC, respectively).

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5 nM for TRKA, 0.7 nM for TRKB, and 2.6 nM for TRKC. The compound demonstrates good selectivity within the kinase group and exhibits significant anti-tumor efficacy in vivo.

Type II TRK Inhibitor 1 is a potent inhibitor targeting multiple tropomyosin receptor kinase (TRK) fusion protein variants as well as the wild type. It demonstrates notable antiproliferative effects on Ba/F3 cells expressing CD74-TRKA G667C and ETV6-TRKC G696C, with half-maximal inhibitory concentrations (IC50s) of 6 nM and 1.7 nM, respectively [1].

TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), with IC50 values of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the mutant TRKA G667C, respectively. It also exhibits IC50 values of 1.3 nM against FLT3, 9.9 nM against RET, and 71.1 nM against VEGFR2. TRK II-IN-1 primarily serves as a research tool for studying TRK-driven cancers [1].

TRK-IN-19 (Compound I-10) is a potent TRK inhibitor with IC50 values of 1.1 nM for TRKA and 5.3 nM for TRKAG595R, demonstrating potential research value in cancer disease.

TRK-IN-16 (WO2012034091A1, compound X-21) is a highly effective TRK inhibitor, targeting protein kinases that are integral to regulating cell growth, differentiation, and various cellular signal transduction processes. This compound shows great potential for research in TRK-related diseases [1].

TRK-IN-23 (compound 24b) is a potent, orally active TRK inhibitor with IC50s of 0.5 nM for TRKA, 9 nM for TRKC, 14 nM for TRKA G595R, 4.4 nM for TRKA F589L, and 4.8 nM for TRKA G667C. It induces apoptosis in Ba F3-TRKAG595R and Ba F3-TRKAG667C cells [1].

TRK-IN-13, a potent inhibitor of TRK, has shown potential for studying TRK-related diseases.

Trk-IN-7 (compound I-6) is a highly potent TRK inhibitor, with IC50 values of 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. It also shows significant inhibition of EML4-ALK (IC50 <15 nM) and ALK mutations G1202R, C1156Y, R1275Q, F1174L, L1197M, and G1269A (IC50 = 5-50 nM) [1].

TRK-IN-14 is a potent TRK inhibitor that has shown potential for treating TRK-related diseases (TRK-IN-13).

Trk-IN-10 (Compound 14j) is a highly effective inhibitor of TRK, with an IC50 of 0.86 nM against TrkA and 6.92 nM against TrkA G595R. As an RTK, Trk is a crucial drug target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) demonstrates superior selectivity in inhibiting Trk, potentially reducing toxicity [1].

TRK-IN-12 (Compound 9e), a macrocyclic derivative, is a potent TRK inhibitor, with efficacy against TRK G595R (IC 50 = 13.1 nM). It demonstrates significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC 50 = 0.080 μM) and exhibits superior inhibitory performance (IC 50 = 0.646 μM) compared to the control agent LOXO-101 in the Ba/F3-LMNA-NTRK1-G595R cell line [1].

TRK-IN-17 is a potent inhibitor of TRK, specifically targeting tropomyosin-related kinase (Trk), a receptor tyrosine kinase activated by neurotrophic factors, which include nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), neurotrophic factor-3 (NT-3), and neurotrophic factor-4 5 (NT-4 5). TRK-IN-17 has potential for cancer disease research.

DDR-TRK-1N is a negative control for DDR-TRK-1.

TRK-IN-24 (compound 10g) is a selective inhibitor of Trk receptors, effectively targeting TRKA, TRKC, and mutant forms TRKA G595R, TRKA G667C, and TRKA F589L, with corresponding IC50 values of 5.21, 4.51, 6.77, 1.42, and 6.13 nM. It demonstrates antitumor activity in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models and inhibits the proliferation of Ba F3 cells expressing single mutants SF, GK, and xDFG, with an IC50 range of 1.43-47.56 nM [1].

Pan-Trk-IN-2 is a small molecule Trks inhibitor that exhibits promising antitumor effects.

Trk-IN-9 (Compound 12) is a potent inhibitor of TRK that inhibits the proliferation of Km-12 cell lines and induces apoptosis in a concentration-dependent manner. It also inhibits TRK phosphorylation and blocks downstream pathways, showing potential for NTRK fusion cancer research.

Trk-IN-6 exhibits exceptional in vitro potency against a range of TRK mutants (IC50 = 0.2-0.7 nM).

TRK-IN-18 is a potent inhibitor of TRK, a family of receptor tyrosine kinases (Trks) activated by neurotrophic factors, which include nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), neurotrophic factor-3 (NT-3), and neurotrophic factor-4 5 (NT-4 5). 18 exhibits potential for the study of cancer diseases.

TRK-380 (TAC-301) is an effective and selective β3-adrenergic receptor agonist. TRK-380 improves formalin-induced frequent urination in rats and carbachol-induced bladder contraction in dogs (a decrease of 37.6%).

Trk-IN-11 (Compound 14h) is a potent TRK inhibitor with IC50 values of 1.4 nM for TrkA and 1.8 nM for TrkA G595R, displaying research potential in cancer diseases.

TRK/ALK-IN-1 is a potent dual inhibitor of TRK and ALK, exhibiting good correlation between its enzymatic inhibition and anti-proliferative activities, with IC50 values of 2.2 nM for TRKA, 9.3 nM for ALK WT, and 38 nM for ALK L1196M. It holds potential for cancer research applications.

Trk-IN-8, a powerful TRK inhibitor, demonstrates excellent potency against TRKAa, TRKA(G595R), and TRKC(G623R) with IC50 values of 0.42 nM, 0.89 nM, and 1.5 nM, respectively (WO2021115401A1, compound 3) [1].

Trk-IN-20 is a 3-vinylindazole derivative compound that effectively inhibits the functions of Trk kinases. It accomplishes this by suppressing the phosphorylation of TrkA, TrkB, and TrkC, with IC50 values of 1.6 nM, 2.9 nM, and 2.0 nM, respectively [1].

TRK-IN-21 (5n) is an orally active TRK inhibitor that acts on TRKAWT (IC50: 0.3 nM), TRKAG667C (IC50: 2.3 nM), TRKAF589L (IC50: 0.4 nM), and TRKAG595 (IC50: 0.5 nM). TRK-IN-21 can be used to study cancer.

TRK-IN-15 (WO2012034091A1, compound X-55) is a highly effective inhibitor of TRK, a protein kinase with crucial involvement in the regulation of cellular growth, differentiation, and signal transduction. Offering significant potential for studying TRK-related diseases, TRK-IN-15 holds promise for advancing research in this field [1].

Pan-Trk-IN-3 is a potent, broad-spectrum inhibitor of Trk and its drug-resistant mutants, acting on TrkA (IC50: 2 nM), TrkB (IC50: 3 nM), TrkC (IC50: 2 nM), TrkAG595R (IC50: 21 nM), TrkAG667C (IC50: 26 nM), TrkAG667S (IC50: 5 nM), TrkAF589L (IC50: 7 nM) and TrkCG623R (IC50: 6 nM), TrkAG667S (IC50: 5 nM), TrkAF589L (IC50: 7 nM) and TrkCG623R (IC50: 6 nM). Pan-Trk-IN-3 induces apoptosis and has significant anti-tumour effects.

Naltalimide is a unique µ-opioid receptor partial agonist. Naltalimide also enhances the bladder storage function by modulating the afferent limb of the micturition reflex through µ-opioid receptors in the spinal cord.

N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) , also known as Normelatonin, is the immediate precursor of melatonin. It is produced from serotonin by the enzyme aralkylamine N-acetyltransferase and is converted to melatonin by acetylserotonin O-methyltransferase. It can potently activate TrkB receptor.

7,8-Dihydroxyflavone (7,8-DHF) is a naturally-occurring flavone and exist in Tridax procumbens, Godmania aesculifolia, and primula tree leaves.

Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

CG 428 is a potent tropomyosin receptor Kinase (TRK) Degrader (uSMITETM) with a DC50 of 0.36 nM. CG 428 comprises an analog of the pan-TRK inhibitor GNF-8625 joined by a linker to the cereblon E3 ligase ligand pomalidomide. CG 428 shows selectivity for TRKA over TRKC and TRKB with Kds of 1nM, 4.2 nM, and 28 nM. CG 428 inhibits the growth of KM12 colon cancer cells with an IC50 of 2.9 nM.

GNF-8625 monopyridin-N-piperazine hydrochloride is a tropomyosin receptor kinase (TRK) inhibitor.

TrkA-IN-1 is a potent and selective inhibitor of Tropomyosin-related kinase A (TrkA) [IC50: 99 nM in a cell-based assay] with analgesic activity.

hTrkA-IN-2 is a selective inhibitor of hTrkA metamorphosis, with an IC50 of 3.9 nM.

TrkA-IN-4, a potent and orally active allosteric TrkA inhibitor, is a prodrug of TrkA-IN-3 and exhibits potent antinociceptive effects [1].

TrkB-IN-1 is a potent, orally active agonist of the TrkB receptor, with favorable pharmacokinetic (PK) properties. It has been shown to reverse cognitive deficits in an Alzheimer's disease (AD) mouse model, thus serving as a valuable tool for Alzheimer’s disease research [1].

hTrkA-IN-1 is a potent and orally active inhibitor of TrkA kinase with an IC 50 of 1.3 nM, compound 2.hTrkA-IN-1 can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al.

FLT3 TrKA-IN-1 is a potent dual kinase inhibitor that targets FLT3 (IC50: 43.8 nM), FLT3-ITD (IC50: 97.2 nM), FLT3-TKD (IC50: 92.5 nM), and TrKA (IC50: 23.6 nM). FLT3 TrKA-IN-1 shows potential for acute myeloid leukaemia (AML) studies.

ITK TRKA-IN-1 is a chemical compound that functions as 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, it effectively inhibits ITK activity and demonstrates a remarkable 96% inhibition of TRKA.

TrkA-IN-3 is a potent, subselective, and allosteric inhibitor of TrkA with an IC50 of 22.4 nM, demonstrating over 8000-fold selectivity towards TrkA compared to TrkB and TrkC, making it valuable for pain research.

GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA TrkB (IC50: 8 12 nM).

Repotrectinib (TPX-0005) is a potent ALK ROS1 TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.

Echinacoside is a natural polyphenolic compound with various kinds of pharmacological activities, such as anti-inflammatory, antioxidative, hepatoprotective, neuroprotective, nitric oxide radical-scavenging and vasodilative ones.

Selitrectinib (LOXO-195) is a potent and selective inhibitor of receptor tyrosine kinases TRK (TrkA and TrkC) with IC50 values of 0.6 nM and <2.5 nM, respectively.