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 A,FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
-
Cancer Cell, 2024, 42(4):535-551.e8
-
Nat Commun, 2024, 15(1):2581
-
Nat Commun, 2024, 15(1):987
|
|
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. |
-
Front Cell Neurosci, 2024, 18:1441827
-
Mol Neurodegener, 2023, 18(1):31
-
Mol Neurodegener, 2023, 18(1):31
|
|
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. |
-
Signal Transduct Target Ther, 2024, 9(1):153
-
Biomed Pharmacother, 2024, 176:116766
-
J Pathol, 2024, 263(2):257-269
|
|
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
|
|
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.
|
-
Alzheimers Dement, 2024, 10.1002/alz.13819
-
Theranostics, 2024, 14(6):2345-2366
-
Cell Commun Signal, 2024, 22(1):309
|
|
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. |
-
Oncogenesis, 2023, 12(1):8
-
Front Pharmacol, 2022, 13:1032975
-
Molecules, 2022, 27(19)6500
|
|
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. |
-
Cells, 2023, 12(3)373
-
Cells, 2023, 12(3):373
-
J Cell Mol Med, 2023, 10.1111/jcmm.17906
|
|
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 Med, 2024, 13(12):e7393
-
Front Pharmacol, 2022, 13:1032975
-
J Cell Mol Med, 2022, 26(21):5539-5550
|
|
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). |
-
Commun Biol, 2024, 7(1):412
-
Cancer Discov, 2023, 13(3):598-615
-
EMBO Mol Med, 2023, 10.15252/emmm.202217367
|
|
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. |
-
Sci Rep, 2024, 14(1):22191
-
Transl Lung Cancer Res, 2022, 11(11:2216-2229)
-
Mol Cancer Ther, 2021, 20(9):1653-1662
|
|
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. |
-
JCI Insight, 2022, e148717
-
Cancers (Basel), 2021, 13(21)5474
-
Cancers (Basel), 2020, 12(1)
|
|
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. |
-
Sci Signal, 2023, 16(787):eadf6696
-
Molecules, 2022, 27(19)6500
-
Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-3165
|
|
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
|
|
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. |
|
|
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 A,FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
- Cancer Cell, 2024, 42(4):535-551.e8
- Nat Commun, 2024, 15(1):2581
- Nat Commun, 2024, 15(1):987
|
|
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. |
- Front Cell Neurosci, 2024, 18:1441827
- Mol Neurodegener, 2023, 18(1):31
- Mol Neurodegener, 2023, 18(1):31
|
|
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. |
- Signal Transduct Target Ther, 2024, 9(1):153
- Biomed Pharmacother, 2024, 176:116766
- J Pathol, 2024, 263(2):257-269
|
|
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
|
|
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. |
- Oncogenesis, 2023, 12(1):8
- Front Pharmacol, 2022, 13:1032975
- Molecules, 2022, 27(19)6500
|
|
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. |
- Cells, 2023, 12(3)373
- Cells, 2023, 12(3):373
- J Cell Mol Med, 2023, 10.1111/jcmm.17906
|
|
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 Med, 2024, 13(12):e7393
- Front Pharmacol, 2022, 13:1032975
- J Cell Mol Med, 2022, 26(21):5539-5550
|
|
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). |
- Commun Biol, 2024, 7(1):412
- Cancer Discov, 2023, 13(3):598-615
- EMBO Mol Med, 2023, 10.15252/emmm.202217367
|
|
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. |
- Sci Rep, 2024, 14(1):22191
- Transl Lung Cancer Res, 2022, 11(11:2216-2229)
- Mol Cancer Ther, 2021, 20(9):1653-1662
|
|
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. |
- JCI Insight, 2022, e148717
- Cancers (Basel), 2021, 13(21)5474
- Cancers (Basel), 2020, 12(1)
|
|
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. |
- Sci Signal, 2023, 16(787):eadf6696
- Molecules, 2022, 27(19)6500
- Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-3165
|
|
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
|
|
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).
"
|
|
|