f-627

Efbemalenograstim alfa (F 627) is a recombinant fusion protein consisting of a long-acting dimeric granulocyte colony-stimulating factor (G-CSF) with two human G-CSF molecules linked by a peptide to a human immunoglobulin G2 (hIgG2)-Fc fragment, designed to induce white blood cell production [1].

MORF-627 is an orally active selective inhibitor of integrin αvβ6 (integrinαvβ6), with an IC50 of 9.2 nM as measured in a human serum ligand binding assay. It effectively inhibits αvβ6-mediated activation of TGF-β1 with an IC50 of 2.63 nM and suppresses SMAD2/3 phosphorylation, showing an IC50 of 8.3 nM. Additionally, MORF-627 ameliorates bleomycin-induced pulmonary fibrosis in mice.

PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and 6.6 nM, respectively.

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).

PF-06278121 is a potent and selective Trk inhibitor. PF-06278121 shows Trk A/B IC50 = 4/94 nM (enzymatic assay), Trk A/B/C IC50 = 13/7/6 nM (PathHunter cell assay).