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全部(82) Agonist(2) Antagonist(1) Inhibitor(7) Activator(2)
Belizatinib 是一种有效的、口服可用的双重ALK和TRK抑制剂,对野生型重组ALK的IC50值为0.7 nM。
Entrectinib(NMS-E628)是一种口服有效的、可穿透血脑屏障的TrkA/B/C、ROS1和ALK抑制剂,对它们的IC50值分别为1、3、5、12和7 nM。它在癌细胞中诱导凋亡和细胞周期停滞,显示出抗肿瘤活性,并减轻小鼠中博来霉素引起的肺纤维化。
ANA-12 is antagonist of TrkB with Kd of 10 nM.
LOXO-195 is a TRK kinase inhibitor (TKI) with IC50 values of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively.
LM22B-10 is an agonist of TrkB and TrkC neurotrophin receptor. It can improve survival and increase neurite outgrowth in vitro.
GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively).
GW 441756 is an inhibitor of tropomyosin-related kinase A (TrkA) with IC50 of 2 nM.
LM22A-4 is a specific agonist oftyrosine kinase receptor B.
LOXO-101 is an ATP-competitive inhibitor of TRK with IC50 of nanomolar range for all the family members.
TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.
Altiratinib is a c-MET/TIE-2/VEGFR inhibitor which effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.
CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
7,8-Dihydroxyflavone acts as an agonist of TrkB receptor with Kd of 320 nM with neuroprotective effect.
LOXO-101 sulfate blocks the ATP binding site of the TRK family of receptors with IC50 of 2 nM to 20 nM against TRKA, TRKB, and TRKC.
Tags: Trk受体 | Trk Receptor | 神经信号通路 | Neuronal Signaling | 蛋白质酪氨酸激酶(Protein Tyrosine Kinase) | Protein Tyrosine Kinase/RTK | Trk受体 相关产品
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