Trk receptor Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S6760 | LM22B-10 | 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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| S6412 | Altiratinib | Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 values 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. |
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| 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. |
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| 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, kinase-selective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively. | ||
| 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. |
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| 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. |
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| 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). |
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| 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. |
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| S8901 | Taletrectinib (DS-6051b) | Taletrectinib (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. |
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| 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. |
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| 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). |
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