- TrkA
- TrkB
- TrkC
TrkB 选择性抑制剂 | 激活剂 | 激动剂 | 拮抗剂
| 目录号 | 产品名 | 产品描述 | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| 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. |
Selective | |
| 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. | Selective | TrkB, Kd: 10 nM |
| 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). | Selective | TrkB receptor, Kd: 320 nM |
| 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. | Selective | |
| 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. | Pan | TrkB, IC50: 2.28 nM |
| 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. | Pan | TrkB, IC50: 4 nM |
| 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. | Pan | TrkB, IC50: 4.1 nM |
| 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. | Pan | TrkB, IC50: 4.6 nM |
| 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. | Pan | TrkB, IC50: 7.8 nM |
| 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. | Pan | TRKB (NTRK2), IC50: 9 nM |
| 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. | Pan | TrkB, IC50: 12 nM |
| 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. | Pan | TrkB, IC50: 100 nM |
| 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. | Pan | |
| 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. | Pan | |
| 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). " | Pan |
