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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

Trk receptor

Trk receptors are a family of tyrosine kinases that regulates synaptic strength and plasticity in the mammalian nervous system. Trk receptors affect neuronal survival and differentiation through several signaling cascades.The common ligands of trk receptors are neurotrophins, a family of growth factors critical to the functioning of the nervous system. The binding of these molecules is highly specific. Each type of neurotrophin has different binding affinity toward its corresponding Trk receptor. The activation of Trk receptors by neurotrophin binding may lead to activation of signal cascades resulting in promoting survival and other functional regulation of cells.

Filter HomeSignaling PathwaysTyrosine Kinase/AdaptorsTrk receptor

Tepotinib

T61211100598-32-0

Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer.

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7,8-Dihydroxyflavone

T281638183-03-8

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

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Entrectinib

T36781108743-60-7

Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1 3 5 12 7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.

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SP600125

T3109129-56-6

SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40 40 90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.

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CE-245677

T14921717899-97-3

CE-245677 is a potent, reversible inhibitor of Tie2 and TrkA B kinases, with cellular IC50 values of 4.7 nM and 1 nM, respectively.

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CG 428

T412242412055-93-5In house

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.

$178

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ENT-C225

T733972919962-53-9In house

ENT-C225 is a potent TrkB neurotrophin receptor (TrkBR) activator with neuroprotective activity for the study of Alzheimer's disease and Parkinson's disease.

$195

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URMC-099

T60571229582-33-5

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

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Larotrectinib

T59951223403-58-4

Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).

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Repotrectinib

T40711802220-02-5

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.

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Diosmetin

T1704520-34-3

Diosmetin (Luteolin 4-methyl ether) has been found to act as a weak TrkB receptor agonist.

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Danusertib

T2094827318-97-8

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.

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ANA-12

T2359219766-25-3

ANA-12 is a potent and selective TrkB antagonist that exhibits anxiolytic and antidepressant activity in mice.

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Sitravatinib

T43491123837-84-2

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

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N-Acetyl-5-hydroxytryptamine

T13541210-83-9

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.

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PF-06273340

T196491402438-74-7

PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10 6 cm s 1).

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LM22A-4

T756837988-18-4

LM22A-4 is a brain-derived neurotrophic factor (BDNF) mimetic and agonist of the receptor tropomyosin-related kinase B (TrkB; IC50 : 47 nM in a fluorescence anisotropy assay)

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GW 441756

T6052504433-23-2

GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.

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Lestaurtinib

T15738111358-88-4

Lestaurtinib (CEP 701) is an orally available and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3, IC50: 0.9 nM), which inhibits FLT3 autophosphorylation in vitro.Lestaurtinib promotes the expression of c-MYC, inhibits the phosphorylation of RPTKs, and has high affinity for TrkA and JAK2. Lestaurtinib promotes c-MYC expression, inhibits phosphorylation of RPTKs, has a high affinity for TrkA and JAK2, induces apoptosis and cell growth arrest, and can be used to study leukemia.

$499

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Milciclib

T6081802539-81-7

Milciclib (PHA-848125) (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.

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Ensartinib hydrochloride

T223242137030-98-7

Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.

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Belizatinib

T42571357920-84-3

Belizatinib (TSR-011) is an effective, oral and dual inhibitor of ALK (IC50: 0.7 nM, wild-type recombinant ALK) and TRKA, TRKB, and TRKC.

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LOXO-195

T94961350884-56-8

(6RS)-LOXO-195 (BAY 2731954) is a potent and selective Trk tyrosine kinase inhibitor.

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Taletrectinib

T223181505515-69-4

Taletrectinib (AB-106) is a new-generation selective inhibitor of ROS1 NTRK including ROS1,NTRK1,NTRK2 and NTRK3 with IC50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM, respectively.

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Altiratinib

T20541345847-93-9

Altiratinib (DCC-2701)(DCC-2701) is a novel c-MET TIE-2 VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with an HGF antagonist in vitro.

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BMS-754807

T23491001350-96-4

Dual IGF-1R InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.

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GNF-8625 monopyridin-N-piperazine hydrochloride

T400342412055-62-8In house

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

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Larotrectinib sulfate

T68801223405-08-0

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

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GNF-5837

T60971033769-28-6

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

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AZ-23

T14363915720-21-7

AZ-23 is an inhibitor of ATP-competitive and Trk kinase A B C. For TrkA, TrkB, FGFR1, Flt3, Ret, MuSk, Lck, the IC50s values are 2 nM, 8 nM, 24 nM, 52 nM, 55 nM, 84 nM, 99 nM, respectively.

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Paltimatrectinib

T624472353522-15-1

Paltimatrectinib (PBI-200) is a potent tyrosine kinase inhibitor with anticancer activity that inhibits myosin-related kinase A (TrkA).Paltimatrectinib is used in the study of bladder, breast and colorectal cancers.

$199

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LM22B-10

T4496342777-54-2

LM22B-10, an activator of the TrkB TrkC neurotrophin receptor, can induce activation of TrkB, TrkC, ERK, and AKT both in vitro and in vivo.

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ONO-7475

T83271646839-59-9

ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase

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Amitriptyline hydrochloride

T0678549-18-8

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

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CH7057288

T56352095616-82-1

CH7057288 is an effective and selective TRK inhibitor with an IC50 value of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB and TRKC, respectively.

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Selitrectinib

T74352097002-61-2

Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively).

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Tyrphostin AG 879

T6712148741-30-4

Tyrphostin AG 879 (AG 879) effectively inhibits HER2 ErbB2 with an IC50 of 1 μM, demonstrating 100- and 500-fold higher selectivity for ErbB2 over EGFR and PDGFR, respectively.

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Cyclotraxin B acetate(1203586-72-4 free base)

TP2068L

Cyclotraxin B acetate is an antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic properties in mice.

$173

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ALE-0540

T9292234779-34-1In house

ALE-0540 is a nonpeptidic heterocyclic molecule that inhibits the binding of NGF to p75 and TrkA, as well as signal transduction and biological responses mediated by TrkA receptors.

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Trk-IN-9

T628062758623-12-8

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.

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Tavilermide

T17000263251-78-1

Tavilermide (MIM-D3) is a selective TrkA agonist, a cyclic mimetic, which can be used to study dry keratoconjunctivitis and dry eye syndrome.

$447

6-8 weeks

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PF-03814735

T6936942487-16-3

PF-03814735 is a novel, potent and reversible inhibitor of Aurora A B with IC50of 0.8 nM 5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.

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Trk-IN-4

T171691799788-94-5In house

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).

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Multi-kinase-IN-6

T81740

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX cancer cell lines with IC50s of 3.36 μM, 1.40 μM, and 3.49 μM, respectively. Additionally, Multi-kinase-IN-6 induces cell cycle arrest at the G1 S and G1 phases in MCF7 and HCT116 cells, respectively, and effectively triggers apoptosis [1].

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TRK II-IN-1

T730332904690-41-9

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].

$1,520

6-8 weeks

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NMS-P626

T200149942471-37-6

NMS-P626 functions as an inhibitor targeting TRKA, TRKB, and TRKC, exhibiting IC 50 values of 8 nM, 7 nM, and 3 nM respectively. It effectively suppresses KM12 cell growth by inhibiting the phosphorylation of TPM3-TRKA and the subsequent downstream signaling, demonstrating an IC 50 of 19 nM specifically for KM12 cells. This compound is applicable in the study of colorectal cancer.

$2,420

10-14 weeks

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TrkA-IN-1

T132081680179-43-4

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.

$1,100

6-8 weeks

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Type II TRK inhibitor 1

T722892937543-72-9

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].

$1,370

8-10 weeks

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