Biological Activity:

GNF-7 is a potent, selective and bioavailable Ras signaling inhibitor. It inhibits Ack1 and germinal center kinase (GCK). It can suppress proliferation, and induce cell cycle arrest and apoptosis in leukemia cells harboring NRAS mutations. In vivo GNF-7 showed good efficacy in a xenotransplantation model and activity against primary AML patient samples.

How to Use:

In vitro: GNF-7 was used at 1 µM final concentration in vitro and in cellular assays.
In vivo: GNF-7 was orally dosed to MOLT-3 xenotransplantation model at 7.5-15 mg/Kg once a day.

Reference:

• 1. Nonami A., et al. Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach. (2015) Blood. 125(20):3133-43.