alk-in-6

ALK-IN-6 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK, IC50s: 71 nM, 18.72 nM, and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L).

CEP-28122 mesylate salt (1022958-60-6 free base) 是一种高选择性的口服活性 ALK 抑制剂(在基于酶的 TRF 测定中，IC50：1.9 nM)。

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].

Zilurgisertib fumarate (INB-000928 fumarate) 是一种高效且选择性的激活素受体样激酶 2 (ALK2/ACVR1) 抑制剂。它能够显著抑制 ALK2 的激酶活性（IC50 = 15 nM），并下调由 BMP-6 诱导的 SMAD1/5 磷酸化（IC50 = 63 nM）。Zilurgisertib 通过阻断 ALK2 介导的信号传导，可抑制肝细胞中铁调素 (hepcidin) 的产生（IC50 = 20 nM），从而调节铁代谢。在临床前研究中，Zilurgisertib 在癌症诱发贫血模型中展现出改善贫血的潜力，能有效增加血红蛋白水平。