trk-in-6

Trk-IN-6 exhibits exceptional in vitro potency against a range of TRK mutants (IC50 = 0.2-0.7 nM).

PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10 6 cm s 1).

Trk-IN-7 (compound I-6) is a highly potent TRK inhibitor, with IC50 values of 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. It also shows significant inhibition of EML4-ALK (IC50 <15 nM) and ALK mutations G1202R, C1156Y, R1275Q, F1174L, L1197M, and G1269A (IC50 = 5-50 nM) [1].

Pan-Trk-IN-3 is a potent, broad-spectrum inhibitor of Trk and its drug-resistant mutants, acting on 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) and TrkCG623R (IC50: 6 nM), TrkAG667S (IC50: 5 nM), TrkAF589L (IC50: 7 nM) and TrkCG623R (IC50: 6 nM). Pan-Trk-IN-3 induces apoptosis and has significant anti-tumour effects.