Trk receptor

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Trk receptor Products

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Catalog No. Product Name Information Product Use Citations Product Validations
E2390New Thalidomide-5-NH2-CH2-COOH Thalidomide-5-NH2-CH2-COOH is a potent and selective inhibitor of tropomyosin receptor kinase (Trk).
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. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Environ Mol Mutagen, 2022, 63(3):151-161
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Front Oncol, 2021, 11:650052
Life Sci, 2021, 267:118977
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nature, 2022, 604(7904):146-151
Cancer Cell, 2022, S1535-6108(21)00662-0
Immunity, 2022, 55(7):1185-1199.e8
S2891 GW441756 GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.
Microbes Infect, 2022, S1286-4579(22)00050-8
Biosci Biotechnol Biochem, 2021, 85(3):675-686
Cancer Res, 2020, canres.1992.2020
S5860 Larotrectinib Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors.
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
Int J Mol Sci, 2021, 23(1)395
Journal of Cancer, 2021, 12(21): 6356-6362
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. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S7519 GNF-5837 GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively.
Clin Transl Oncol, 2021, 10.1007/s12094-021-02666-x
Oncol Rep, 2019, 42(5):2039-2048
Cancer Cell, 2018, 34(2):315-330
S7960 Larotrectinib (LOXO-101) sulfate Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
Int J Mol Sci, 2021, 23(1)395
J Neuropathol Exp Neurol, 2021, nlab016
S7998 Entrectinib (RXDX-101) Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cancer Res, 2022, canres.1397.2021
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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 the compound is between 5- and 67-fold selective.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
ScholarsArchive@OSU, 2020, 51
ScholarsArchive@OSU, 2020, None
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.
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). "
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.
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
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); also a potent SRC inhibitor (IC50 5.3 nM).
Cancer Res, 2022, canres.1397.2021
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2020, clincanres.2585.2020
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. It is more than 1,000-fold selective for 98% of non-TRK kinases tested.
Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-3165
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.
S8901 Taletrectinib (DS-6051b) Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.
Mol Cancer Ther, 2021, molcanther.0965.2020
Mol Cancer Ther, 2021, 20(9):1653-1662
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
JCI Insight, 2022, 7(7)e154824
Front Immunol, 2020, 11:564133
Cell Signal, 2014, 26(1):149-61
S6760 LM22B-10 LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.
S7745 ANA-12 ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.
FASEB J, 2022, 36(4):e22263
Mol Neurobiol, 2022, 10.1007/s12035-022-02757-y
Pharmacol Res, 2022, 176:106079
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.
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.

S8319 7,8-Dihydroxyflavone 7,8-Dihydroxyflavone (7,8-DHF) acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF).
Pharmacol Res, 2022, 176:106079
Neuropharmacology, 2021, 196:108717
J Biochem Mol Toxicol, 2021, e22775
E2390New Thalidomide-5-NH2-CH2-COOH Thalidomide-5-NH2-CH2-COOH is a potent and selective inhibitor of tropomyosin receptor kinase (Trk).
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. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Environ Mol Mutagen, 2022, 63(3):151-161
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Front Oncol, 2021, 11:650052
Life Sci, 2021, 267:118977
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nature, 2022, 604(7904):146-151
Cancer Cell, 2022, S1535-6108(21)00662-0
Immunity, 2022, 55(7):1185-1199.e8
S2891 GW441756 GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.
Microbes Infect, 2022, S1286-4579(22)00050-8
Biosci Biotechnol Biochem, 2021, 85(3):675-686
Cancer Res, 2020, canres.1992.2020
S5860 Larotrectinib Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors.
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
Int J Mol Sci, 2021, 23(1)395
Journal of Cancer, 2021, 12(21): 6356-6362
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. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S7519 GNF-5837 GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively.
Clin Transl Oncol, 2021, 10.1007/s12094-021-02666-x
Oncol Rep, 2019, 42(5):2039-2048
Cancer Cell, 2018, 34(2):315-330
S7960 Larotrectinib (LOXO-101) sulfate Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
Int J Mol Sci, 2021, 23(1)395
J Neuropathol Exp Neurol, 2021, nlab016
S7998 Entrectinib (RXDX-101) Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cancer Res, 2022, canres.1397.2021
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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 the compound is between 5- and 67-fold selective.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
ScholarsArchive@OSU, 2020, 51
ScholarsArchive@OSU, 2020, None
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.
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). "
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.
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
Cancers (Basel), 2020, 12(1)
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); also a potent SRC inhibitor (IC50 5.3 nM).
Cancer Res, 2022, canres.1397.2021
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2020, clincanres.2585.2020
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. It is more than 1,000-fold selective for 98% of non-TRK kinases tested.
Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-3165
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.
S8901 Taletrectinib (DS-6051b) Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.
Mol Cancer Ther, 2021, molcanther.0965.2020
Mol Cancer Ther, 2021, 20(9):1653-1662
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
S9662 UNC2025 UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.
JCI Insight, 2022, 7(7)e154824
Front Immunol, 2020, 11:564133
Cell Signal, 2014, 26(1):149-61
S6760 LM22B-10 LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator, LM22B-10 selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.
S7745 ANA-12 ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.
FASEB J, 2022, 36(4):e22263
Mol Neurobiol, 2022, 10.1007/s12035-022-02757-y
Pharmacol Res, 2022, 176:106079
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.
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.

S8319 7,8-Dihydroxyflavone 7,8-Dihydroxyflavone (7,8-DHF) acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF).
Pharmacol Res, 2022, 176:106079
Neuropharmacology, 2021, 196:108717
J Biochem Mol Toxicol, 2021, e22775
E2390New Thalidomide-5-NH2-CH2-COOH Thalidomide-5-NH2-CH2-COOH is a potent and selective inhibitor of tropomyosin receptor kinase (Trk).
Tags: Trk receptor inhibitor|Trk receptor agonist|Trk receptor activator|Trk receptor inducer|Trk receptor antagonist|Trk receptor signaling pathway|Trk receptor assay kit