Cayman Vu0364439; Size- 5 Mg

GNF-7 is a multi-kinase inhibitor (IC₅₀s = 25, 8, 61, 122, 136, and 133 nM for ACK1, GCK, Bcr-Abl^T315I, Bcr-Abl^E255V, Bcr-Abl^G250E, and c-Abl, respectively).^, It also inhibits several additional kinases in a panel by greater than 50% when used at a concentration of 10 μM. GNF-7 inhibits the growth of Ba/F3 cells transformed with wild-type Bcr-Abl, Bcr-Abl^T315I, Bcr-Abl^E255V, and Bcr-Abl^G250E (IC₅₀s = <5 nM), as well as COLO 205 and SW625 cancer cells (IC₅₀s = 1 and 5 nM, respectively) in vitro. In vivo, GNF-7 (10 and 20 mg/kg) reduces tumor growth in a Bcr-Abl^T315I Ba/F3 mouse xenograft model. It also reduces tumor volume in an OCI-AML3 mouse xenograft model when administered at a dose of 8 mg/kg.

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