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Description: GNF-7 is a novel, potent, oral bioactive type-II kinase Bcr-Abl inhibitor with IC50 of<5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
References: J Med Chem. 2010 Aug 12;53(15):5439-48; Blood. 2015 May 14;125(20):3133-43.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), GNF-7 also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. GNF-7, potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK.
Kinase Assay: GNF-7 is amongst the first type II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design next generation Bcr-Abl kinase inhibitors. GNF-7 exhibits some selectivity (4 to 100-fold) for T315I Bcr-Abl (IC50 = 11 nM, in Ba/F3 cell line) relative to kinases such as TPR-Met, NPM-ALK, JAK-3, Flt-3.
Purity ≥ 98%
COA
MSDS
Effect of GNF-7 suppression of AKT and/or GCK on induction of apoptosis and cell cycle. Blood. 2015 May 14; 125(20): 3133–3143.
In vivo efficacy of GNF-7 in a xenotransplantation model and activity against primary AML patient samples. Blood. 2015 May 14; 125(20): 3133–3143.
Identification of GCK as a functionally relevant target of GNF-7. Blood. 2015 May 14;125(20):3133-43.