Drug intelligence / Profile preview

gnf-7

Development stage
Preclinical
Lead developer
ActivX Biosciences
Modality
Small Molecules
Administration
Oral
01

Overview

GNF-7 is a **multikinase inhibitor** that acts as a potent, orally bioavailable type II kinase inhibitor targeting several clinically relevant kinases, most notably **Bcr-Abl (including T315I mutation)**, **FLT3-ITD**, and **NRAS-dependent signaling pathways**[1][3][4][5][7][9]. GNF-7 inhibits mutant forms of Bcr-Abl resistant to other tyrosine kinase inhibitors (TKIs), including T315I, and shows potent activity against FLT3-ITD and FLT3-ITD/F691L mutations, implicated in drug resistance in acute myeloid leukemia (AML)[1][4][7]. It also inhibits **activated CDC42 kinase 1 (ACK1)** and **germinal center kinase (GCK)**[7][9]. GNF-7 inhibits cellular proliferation in various cancer models, induces cell cycle arrest and apoptosis, and suppresses key downstream pathways (such as STAT5, PI3K/AKT, and MAPK/ERK)[1][4]. Developed initially by **ActivX Biosciences**, GNF-7 is primarily in the preclinical research phase as a lead compound for hematologic and solid tumors, particularly **drug-resistant leukemias**, but also shows anti-proliferative effects against BRAF mutant cancers[5].

Other names
N-[3-[1,4-dihydro-1-methyl-7-[(6-methyl-3-pyridinyl)amino]-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide
02

Targets

TNK2 (Activated Cdc42-associated kinase 1)CSK (C-terminal Src kinase)GCK (Glucokinase)LYN (LYN proto-oncogene, Src family tyrosine kinase)FLT3-ITD (Fms-like tyrosine kinase 3 with internal tandem duplication)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)LCK (Proto-oncogene tyrosine-protein kinase Lck)

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