Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Deltarasin selectively binds to the prenyl-binding pocket of PDEδ with nanomolar affinity (IC50 = 41 nM, binding to PDEδ in cell). Deltarasin was tested as an inhibitor in mice that had previously received injections of human tumor cells with KRAS mutations. Deltarasin was effective as an inhibitor in sharply reducing tumor growth in comparison to a placebo.
|Animal models||Mice bearing Panc-Tu-I xenografts|
|Formulation||Lipovenoes 10% PLR and 5% DMSO|
|Dosages||10 mg/kg bid|
|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.
Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site.
Zimmermann G, et al. J Med Chem. 2014 Jun 26;57(12):5435-48. PMID: 24884780.
Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling.
Zimmermann G, et al. Nature. 2013 May 30;497(7451):638-42. PMID: 23698361.
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