GNF-5 is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog.It exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 in murine xenograft models of leukemia.GNF-5 shows potent antiproliferative activity with EC50 of 430 nM and 580 nM against wt-Bcr-Abl and E255K mutant Bcr-Abl transformed cells, respectively. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site 'gatekeeper' mutant T315I.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.
Zhang J,et al. Nature. 2010 Jan 28;463(7280). PMID: 20072125.
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GNF-7 is 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.
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