trk-in-6

Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants ( IC 50 = 0.2-0.7 nM).

PF-06273340 是一种口服具有活力的、具有选择性的外周限制性Trk 泛抑制剂。

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。