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Trk receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S8636 Selitrectinib (LOXO-195) Selitrectinib (LOXO-195, BAY 2731954) is an orally available, highly potent, and selective TRK kinase inhibitor with low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, IC50s ranging from 2.0 to 9.8 nmol/L. This compound is more than 1,000-fold selective for 98% of non-TRK kinases tested.
Molecules, October 1, 2022, 6500
Science Signaling, May 30, 2023, eadf6696
Science Signaling, May 23, 2023, eadf6696
S6412 Altiratinib Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. This compound inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
J Microbiol, 2025, 63(2):e2409001
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S2985 N-Acetyl-5-hydroxytryptamine

N-Acetyl-5-hydroxytryptamine (NAS, N-Acetylserotonin, Normelatonin, O-Demethylmelatonin), a precursor of melatonin, is a potent and selective agonist of TrkB receptor.
iScience, 2023, 26(3):106241
iScience, 2023, 106241
S8788 CH7057288 CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.
Molecular Medicine Reports, 2021, 423
S8407 PF-06273340 PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.
Toxicology and Applied Pharmacology, May 2024, 116945
S0827 LM22A-4 LM22A-4 (LM 22A4) is a specific agonist of tyrosine kinase receptor B (TrkB) that reduces the development of tissue injury associated with spinal cord trauma.
E2390 Thalidomide-5-NH2-CH2-COOH Thalidomide-5-NH2-CH2-COOH is a potent and selective inhibitor of tropomyosin receptor kinase (Trk).
S1124 BMS-754807 BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.
Molecular Cancer Research, September 02 2022, 1405-1419
Acta Pharmacologica Sinica, July 17 2019, 270-277
Cell Reports, August 26 2025, 116149
Verified customer review of BMS-754807
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. It induces apoptosis, cell cycle arrest, and autophagy. This compound is in Phase 2.
Elife, 2024, 12RP92324
Sci Rep, 2024, 14(1):4303
Environ Mol Mutagen, 2024, 10.1002/em.22604
Verified customer review of Danusertib (PHA-739358)
S8583 Repotrectinib (TPX-0005) Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); it is also a potent SRC inhibitor (IC50 5.3 nM).
Cancer Discovery, March 01, 2023, 598-615
Molecular Cancer Therapeutics, July 02, 2025, 1005-1019
npj Precision Oncology, 2025, Online ahead of print
S8573 Sitravatinib (MGCD516) Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
Translational Cancer Research, October 2019, 2425-2438
Cancer Research, October 15, 2025, 3983-3998
Neuro-Oncology, May 2025, 1372–1384
S8901 Taletrectinib (DS-6051b) Taletretinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor, with ic50 values of 0.207 nM, 0.622 nM, 2.28 nM, and 0.980 nM for ROS1, NTRK1, NTRK2, and NTRK3, respectively.
Molecular Cancer Therapeutics, September 2021, 1653-1662
Molecular Cancer Therapeutics, September 01 2021, 1653-1662
Translational Lung Cancer Research, November 2022, 2216-2229
S8348 BMS-935177 BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which this compound is between 5- and 67-fold selective.
iScience, 2021, 24(9):102931
iScience, 2021, 102931
iScience, 2021, 102931
S8511 Belizatinib (TSR-011) "Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). "