| S7998 |
Entrectinib (Rxdx-101)
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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.
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Leukemia, 2025, 10.1038/s41375-025-02682-8
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Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
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Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
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| S5860 |
Larotrectinib (LOXO-101)
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Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors.
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Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
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Toxicol Lett, 2025, 406:31-37
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Cancer Med, 2024, 13(12):e7393
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| S9662 |
UNC2025
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UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. This compound 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.
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iScience, 2024, 27(7):110226
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Commun Biol, 2023, 6(1):916
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Int J Mol Sci, 2023, 10.3390/ijms242115903
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| S1460 |
SP600125
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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. This compound 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. It inhibits autophagy and activates apoptosis.
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Nat Commun, 2025, 16(1):7156
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Adv Sci (Weinh), 2025, 12(28):e2502634
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Adv Sci (Weinh), 2025, 12(36):e00028
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| S7745 |
ANA-12
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ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively.
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Antioxidants (Basel), 2025, 14(3)344
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Geroscience, 2025, 10.1007/s11357-025-01783-7
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Neurochem Res, 2025, 50(4):234
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| S7960 |
Larotrectinib sulfate
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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.
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iScience, 2024, 27(10):110862
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Oncogenesis, 2023, 12(1):8
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Front Pharmacol, 2022, 13:1032975
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| S2891 |
GW441756
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GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. This compound produces a relevant increase of caspase-3 that leads to apoptosis.
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Cell Res, 2025, 10.1038/s41422-025-01098-4
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Neurochem Int, 2025, 191:106072
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Cells, 2023, 12(3)373
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| S8319 |
7,8-Dihydroxyflavone
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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).
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Int J Biol Sci, 2023, 19(16):5204-5217
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International Journal of Biological Sciences, 2023, 5204-5217
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Pharmacol Res, 2022, 176:106079
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| S7519 |
GNF-5837
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GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively.
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J Neurochem, 2025, 169(8):e70194
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Cell Rep, 2022, 41(11):111827
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Clin Transl Oncol, 2021, 10.1007/s12094-021-02666-x
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| S6760 |
LM22B-10
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LM22B-10 is a small molecule TrkB/TrkC neurotrophin receptor co-activator. This compound selectively activates TrkB, TrkC, AKT and ERK in vivo and in vitro.
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Theranostics, 2024, 14(4):1561-1582
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Theranostics, 2024, 1561-1582
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Int J Mol Sci, 2024, 25(4)2408
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