Trk receptor

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Trk receptor製品

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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.
Nat Commun, 2025, 16(1):7156
J Exp Clin Cancer Res, 2025, 44(1):159
J Adv Res, 2025, S2090-1232(25)00038-4
SP600125-S1460W01210140905.gif
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.
Cell Rep, 2025, 44(8):116149
Commun Med (Lond), 2025, 5(1):206
Front Cell Neurosci, 2024, 18:1441827
BMS754807-S112401Y0120140228.gif
S7998 Entrectinib Entrectinib 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.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Entrectinib-S799801W0120190225.gif
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.
Elife, 2024, 12RP92324
Sci Rep, 2024, 14(1):4303
Environ Mol Mutagen, 2024, 10.1002/em.22604
PHA-739358-S1107Z0120141124.gif
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.
Antioxidants (Basel), 2025, 14(3)344
Geroscience, 2025, 10.1007/s11357-025-01783-7
Neurochem Int, 2025, 191:106072
ANA-12-S774501Z0820190226.gif
S7960 Larotrectinib sulfate Larotrectinib sulfate 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.
iScience, 2024, 27(10):110862
Oncogenesis, 2023, 12(1):8
Front Pharmacol, 2022, 13:1032975
Larotrectinib-S796001Z0520180428.gif
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.
Cell Res, 2025, 10.1038/s41422-025-01098-4
Neurochem Int, 2025, 191:106072
Cells, 2023, 12(3)373
GW441756-S289101X0720190327.gif
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.
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Toxicol Lett, 2025, 406:31-37
Cancer Med, 2024, 13(12):e7393
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).
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Commun Biol, 2024, 7(1):412
Cancer Discov, 2023, 13(3):598-615
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).
Int J Biol Sci, 2023, 19(16):5204-5217
Pharmacol Res, 2022, 176:106079
Int J Mol Sci, 2022, 23(24)16205
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.
Cell Rep, 2022, 41(11):111827
Clin Transl Oncol, 2021, 10.1007/s12094-021-02666-x
Oncol Rep, 2019, 42(5):2039-2048
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.
iScience, 2024, 27(7):110226
Commun Biol, 2023, 6(1):916
Commun Biol, 2023, 6(1):916
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,TrkA,TrkB and TrkC,respectively.
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Sci Rep, 2024, 14(1):22191
Transl Lung Cancer Res, 2022, 11(11:2216-2229)
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 the compound is between 5- and 67-fold selective.
iScience, 2021, 24(9):102931
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
ScholarsArchive@OSU, 2020, 51
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.
Commun Biol, 2025, 8(1):1185
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
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.
Neurochem Int, 2025, 191:106072
Sci Signal, 2023, 16(787):eadf6696
Molecules, 2022, 27(19)6500
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.
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
F1591 BDNF Antibody [E17G19]
Behav Brain Res, 2021, 411:113389
F0561 TrkB Antibody [N21K17] TrkB Rabbit mAb detects endogenous levels of total TrkB protein. The antibody does not cross-react with TrkA.
F0535 TrkC Antibody [P17E7] TrkC Rabbit mAb detects endogenous levels of total TrkC protein. The antibody does not cross-react with TrkA or TrkB.
F1138 Pan Trk Antibody [B9H18] Pan Trk Rabbit mAb recognizes endogenous levels of total Pan Trk protein.
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.
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.
E2390 Thalidomide-5-NH2-CH2-COOH Thalidomide-5-NH2-CH2-COOH is a potent and selective inhibitor of tropomyosin receptor kinase (Trk).
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.
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.
Theranostics, 2024, 14(4):1561-1582
Int J Mol Sci, 2024, 25(4)2408
Sci Rep, 2024, 14(1):12090
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). "
A2311 Anti-TrkA / NTRK1 Anti-TrkA / NTRK1 is a non-conjugated, rabbit-derived monoclonal antibody targeting TrkA. MW : 145.5 KD.
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).
Int J Biol Sci, 2023, 19(16):5204-5217
Pharmacol Res, 2022, 176:106079
Int J Mol Sci, 2022, 23(24)16205
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
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.
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.
Nat Commun, 2025, 16(1):7156
J Exp Clin Cancer Res, 2025, 44(1):159
J Adv Res, 2025, S2090-1232(25)00038-4
SP600125-S1460W01210140905.gif
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.
Cell Rep, 2025, 44(8):116149
Commun Med (Lond), 2025, 5(1):206
Front Cell Neurosci, 2024, 18:1441827
BMS754807-S112401Y0120140228.gif
S7998 Entrectinib Entrectinib 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.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Entrectinib-S799801W0120190225.gif
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.
Elife, 2024, 12RP92324
Sci Rep, 2024, 14(1):4303
Environ Mol Mutagen, 2024, 10.1002/em.22604
PHA-739358-S1107Z0120141124.gif
S7960 Larotrectinib sulfate Larotrectinib sulfate 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.
iScience, 2024, 27(10):110862
Oncogenesis, 2023, 12(1):8
Front Pharmacol, 2022, 13:1032975
Larotrectinib-S796001Z0520180428.gif
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.
Cell Res, 2025, 10.1038/s41422-025-01098-4
Neurochem Int, 2025, 191:106072
Cells, 2023, 12(3)373
GW441756-S289101X0720190327.gif
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.
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Toxicol Lett, 2025, 406:31-37
Cancer Med, 2024, 13(12):e7393
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).
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Commun Biol, 2024, 7(1):412
Cancer Discov, 2023, 13(3):598-615
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.
Cell Rep, 2022, 41(11):111827
Clin Transl Oncol, 2021, 10.1007/s12094-021-02666-x
Oncol Rep, 2019, 42(5):2039-2048
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.
iScience, 2024, 27(7):110226
Commun Biol, 2023, 6(1):916
Commun Biol, 2023, 6(1):916
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,TrkA,TrkB and TrkC,respectively.
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Sci Rep, 2024, 14(1):22191
Transl Lung Cancer Res, 2022, 11(11:2216-2229)
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 the compound is between 5- and 67-fold selective.
iScience, 2021, 24(9):102931
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
ScholarsArchive@OSU, 2020, 51
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.
Commun Biol, 2025, 8(1):1185
JCI Insight, 2022, e148717
Cancers (Basel), 2021, 13(21)5474
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.
Neurochem Int, 2025, 191:106072
Sci Signal, 2023, 16(787):eadf6696
Molecules, 2022, 27(19)6500
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.
J Microbiol, 2025, 63(2):e2409001
Theranostics, 2021, 11(20):9918-9936
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
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.
E2390 Thalidomide-5-NH2-CH2-COOH Thalidomide-5-NH2-CH2-COOH is a potent and selective inhibitor of tropomyosin receptor kinase (Trk).
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). "
A2311 Anti-TrkA / NTRK1 Anti-TrkA / NTRK1 is a non-conjugated, rabbit-derived monoclonal antibody targeting TrkA. MW : 145.5 KD.
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.
Theranostics, 2024, 14(4):1561-1582
Int J Mol Sci, 2024, 25(4)2408
Sci Rep, 2024, 14(1):12090
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.
Antioxidants (Basel), 2025, 14(3)344
Geroscience, 2025, 10.1007/s11357-025-01783-7
Neurochem Int, 2025, 191:106072
ANA-12-S774501Z0820190226.gif
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).
Int J Biol Sci, 2023, 19(16):5204-5217
Pharmacol Res, 2022, 176:106079
Int J Mol Sci, 2022, 23(24)16205
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
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.

Trk receptorシグナル伝達経路