GSK923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E). GSK923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. GSK923295 demonstrated significant antitumor activity against solid tumor models, inducing CRs in Ewing sarcoma, rhabdoid, and rhabdomyosarcoma xenografts. GSK923295 exhibits robust, dose-dependent antitumor activity against Colo205 xenografts, including partial and complete regressions at the 125 mg/kg dose.
|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.
Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E inhibition.
Mayes PA, et al. Int J Cancer. 2013 Feb 1;132(3):E149-57. PMID: 22948716.
Initial testing of the CENP-E inhibitor GSK923295A by the pediatric preclinical testing program.
Lock RB, et al. Pediatr Blood Cancer. 2012 Jun;58(6):916-23. PMID: 21584937.
Antitumor activity of an allosteric inhibitor of centromere-associated protein-E.
Wood KW, et al. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. PMID: 20167803.
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