GNF 7
Chemical Name: 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
Purity: ≥98%
Biological Activity
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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach.
Nonami et al.
Blood, 2015;125:3133
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