tropomyosin receptor kinase

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

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.

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

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.

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.

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

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

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.

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.

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

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).

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

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).

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.

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.

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).

TrkA-IN-7 (Compound 4) is an inhibitor of tropomyosin receptor kinase A (TrkA), with a Kd value of 40 μM.

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.

Thalidomide-5-NH2-CH2-COOH (compound 114) is a selective inhibitor of the protomyosin receptor kinase and a ligand for E3 ligase, offering potential for studying various diseases.

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.

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.

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.

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