TPX-0005也已经证实对ROS1激酶(ROS1WT0.07nM和ROS1G2032R0.456nM)和TRK家族有更强的抑制作用(TRKA0.826nM,TRKB0.052nM和TRKC0.096nM)。此外TPX-0005还对NIH3T3LMNA-TRKAG595R细胞中的LMNA-TRKAG595R(IC50<1nM)的磷酸化作用和SRCsubstratepaxillin(IC50107nM)有抑制作用。
(MW <370) than current ROS1 inhibitors. It was specifically designed to overcome resistance mutations. Preclinical studies have shown activity against gatekeeper and solvent mutations, including G2032R, D2033N, L2026M, S1986F/Y, L1951R, and kinases involved in bypass signaling such as focal ...
J. et al. TPX-0005, a novel ALK/ROS1/TRK inhibitor, effectively inhibited a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants. European Journal of Cancer 69, S32–S32, https://doi.org/10.1016/ S0959-8049(16)32675-2 (2016). 31. ...
(MW <370) than current ROS1 inhibitors. It was specifically designed to overcome resistance mutations. Preclinical studies have shown activity against gatekeeper and solvent mutations, including G2032R, D2033N, L2026M, S1986F/Y, L1951R, and kinases involved in bypass signaling such as focal ...