Tocris Bioscience™ GNF 7

Descripción

GNF 7 is a potent Bcr-Abl inhibitor (IC50 values are 61 and 133 nM for T315I and wild-type Bcr-Abl, respectively), inhibiting a range of clinically relevant Bcr-Abl mutants such as T315I, G250E, E255V, F317L and M351T. GNF 7 is also a Ras signaling inhibitor as well as inhibiting Ack1 and germinal center kinase (GCK). GNF 7 induces cell cycle arrest and apoptosis in leukemia cells harboring NRAS mutations, and shows growth inhibitory activity in human colon cancer cells. It prolongs survival in a leukemia cell xenotransplantation model in mice and is orally bioavailable.