|
T14921 |
CE-245677
|
|
Tie-2
,
Trk receptor
|
|
CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases. With a cellular IC50s of 4.7 and 1 nM. |
|
T7568 |
LM22A-4
|
|
Trk receptor
|
|
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) |
|
T5635 |
CH7057288
|
|
Trk receptor
|
|
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. |
|
T14363 |
AZ-23
|
AZ 23,AZ23 |
Trk receptor
|
|
|
|
T6097 |
GNF-5837
|
GNF 5837 |
Trk receptor
,
PDGFR
,
c-Kit
|
|
GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM). |
|
T7435 |
Selitrectinib
|
LOXO-195 |
Trk receptor
|
|
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) |
|
T2359 |
ANA-12
|
ANA 12,ANA12 |
Trk receptor
|
|
ANA-12 is a potent and selective TrkB antagonist with anxiolytic and antidepressant activity in mice. |
|
T6052 |
GW 441756
|
|
Apoptosis
,
Raf
,
Trk receptor
,
CDK
|
|
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM. |
|
T9123 |
DS-1205
|
|
TAM Receptor
|
|
DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro an... |
|
T8327 |
ONO-7475
|
|
Trk receptor
,
TAM Receptor
|
|
ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase |
|
T4496 |
LM22B-10
|
LM22B10 |
ERK
,
Trk receptor
,
Akt
|
|
LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor and can induce TrkB, TrkC, ERK and AKT activation in vitro and in vivo. |
|
T4257 |
Belizatinib
|
TSR-011 |
Trk receptor
,
ALK
|
|
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. |
|
T19649 |
PF-06273340
|
PF 6273340,PF 06273340,PF6273340,PF-6273340 |
Trk receptor
|
|
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 efflu... |
|
T5995 |
Larotrectinib
|
LOXO-101,ARRY-470 |
Apoptosis
,
Trk receptor
|
|
Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors(IC50s = 2-20 nM). |
|
T2054 |
Altiratinib
|
DCC-2701 |
VEGFR
,
Tie-2
,
FLT
,
Trk receptor
,
c-Met/HGFR
|
|
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... |
|
T4071 |
Repotrectinib
|
TPX-0005,TPX 0005,TPX0005 |
Trk receptor
,
ROS
,
Src
,
ALK
,
ROS Kinase
|
|
Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively. |
|
T0678 |
Amitriptyline hydrochloride
|
Amitriptyline HCl,Tryptizol,Domical,Annoyltin |
Trk receptor
,
Sigma receptor
,
5-HT Receptor
,
Serotonin Transporter
,
Sodium Channel
,
Adrenergic Receptor
,
AChR
,
Norepinephrine
,
Histamine Receptor
|
|
Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities. |
|
T6712 |
Tyrphostin AG 879
|
AG 879 |
Apoptosis
,
EGFR
,
Trk receptor
,
HER
,
PDGFR
|
|
Tyrphostin AG 879 (AG 879) effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR. |
|
T3678 |
Entrectinib
|
RXDX-101,NMS-E628 |
Trk receptor
,
ROS
,
ALK
,
Autophagy
,
ROS Kinase
|
|
Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectini... |
|
T40019 |
Thalidomide-5-NH2-CH2-COOH
|
|
Others
|
|
Thalidomide-5-NH2-CH2-COOH (compound 114) is a selective inhibitor of the protomyosin receptor kinase. It is a ligand for E3 ligase and has potential for studying one or more diseases. |
|
T4349 |
Sitravatinib
|
MG516,MGCD516 |
Discoidin Domain Receptor (DDR)
,
VEGFR
,
FLT
,
Trk receptor
,
TAM Receptor
,
c-Kit
,
Ephrin Receptor
|
|
Sitravatinib (MGCD516) (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl. |
|
T6880 |
Larotrectinib sulfate
|
LOXO-101 sulfate,Larotrectinib (LOXO-101) sulfate,Larotrectinib,LOXO-101 (sulfate),ARRY-470,ARRY-470 (sulfate) |
Apoptosis
,
Trk receptor
|
|
Larotrectinib sulfate (LOXO-101 sulfate) is an oral active and specific ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
|
T10984 |
DDR-TRK-1
|
|
Discoidin Domain Receptor (DDR)
|
|
DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family. |
|
T40034 |
GNF-8625 monopyridin-N-piperazine hydrochloride
|
|
Trk receptor
|
|
GNF-8625 monopyridin-N-piperazine hydrochloride is a protomyosin receptor kinase (TRK) inhibitor. |
|
T41224 |
CG 428
|
|
Trk receptor
|
|
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 pomalidom... |
|
T34958 |
TRK-380
|
TAC301,TAC 301,TAC-301,TRK 380,TRK380 |
|
|
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%). |
|
T72289 |
Type II TRK inhibitor 1
|
|
Trk receptor
|
|
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 expres... |
|
T15738 |
Lestaurtinib
|
KT-5555,CEP-701 |
Others
|
|
Lestaurtinib is a multi-kinase inhibitor. It also has effective activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3, and TrkA (IC50s: 0.9, 3, and less than 25 nM). |
|
T73033 |
TRK II-IN-1
|
|
Trk receptor
|
|
TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), demonstrating inhibitory half-maximal inhibitory concentrations (IC50s) of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the muta... |
|
T62561 |
TRK-IN-17
|
|
|
|
TRK-IN-17 is a potent inhibitor of TRK. Among them is promyosin-related kinase (Trks), a member of the receptor tyrosine kinase family, which is activated by neurotrophic factors. Neurotrophic factors are a group of solu... |
|
T63346 |
TRK-IN-18
|
|
|
|
TRK-IN-18 is a potent inhibitor of TRK. Among them are promyosin-related kinases (Trks), a family of receptor tyrosine kinases activated by neurotrophic factors, a group of soluble growth factors containing nerve growth ... |
|
T64296 |
TIY-7
|
|
|
|
TIY-7 is a selective, orally active inhibitor of the promyosin receptor kinase (TRK) enzyme. TIY-7 exhibited anti-tumour effects in a mouse xenograft model. |
|
T71267 |
GNF-8625
|
|
|
|
GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in ... |
|
T79706 |
TRK-IN-24
|
|
Trk receptor
|
|
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 IC50 values of 5.21, 4.51, 6.77, 1.42, and 6.13 nM, resp... |
