Trk-IN-7

Trk-IN-7 (compound I-6) is a highly potent inhibitor of TRK, exhibiting IC50 values ranging from 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. In addition, Trk-IN-7 demonstrates notable inhibition against EML4-ALK (IC50 <15 nM), as well as ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50 = 5-50 nM) [1].

Pan-Trk-IN-3 是一种有效的广谱 Trk 及其耐药突变体抑制剂，能够作用于 TrkA (IC50: 2 nM)、TrkB (IC50: 3 nM)、TrkC (IC50: 2 nM)、TrkAG595R (IC50: 21 nM)、TrkAG667C (IC50: 26 nM)、TrkAG667S (IC50: 5 nM)、TrkAF589L (IC50: 7 nM) 和 TrkCG623R (IC50: 6 nM)。Pan-Trk-IN-3 能够诱导细胞凋亡 (apoptosis)，具有显著的抗肿瘤效果。

TIY-7 是一种选择性、口服具有活力的原肌球蛋白受体激酶 (TRK) 抑制剂。TIY-7 能够抑制 TRKA 酶 (IC50: 2.9 nM)、TRKAG595R 酶 (IC50: 1.1 nM)、TRKAG667C 酶 (IC50: 0.7 nM)、TRKAF589L 酶 (IC50: 0.8 nM)、TRKCG623R 酶 (IC50: 0.8 nM)、TRKCG696A 酶 (IC50: 0.2 nM)。TIY-7 在小鼠异种移植模型中表现出抗肿瘤效果。