RO-3306 inhibits CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D activity with Ki of 35 nM, 110 nM, 340 nM, and over 2000 nM, respectively. Treatment of HCT116, SW480, and HeLa cells with RO-3306 for 20 h leads to a complete block of the cell cycle in the G2/M phase. The proliferation of both HCT116 and SW480 is effectively blocked by RO-3306. RO-3306 appears to be more proapoptotic in cancer cells (HCT116 and SW480) than nontumorigenic cells (MCF 10A and MCF 12A). RO-3306 effectively arrests oocyte maturation at a concentration of 10 μM.
|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.
|Solubility||13 mg/mL warmed in DMSO|
RO-3306 prevents postovulatory aging-mediated spontaneous exit from M-II arrest in rat eggs cultured in vitro.
Prasad S, et al. Biomed Pharmacother. 2016 Mar;78:216-25. PMID: 26898445.
A specific inhibitor of CDK1, RO-3306, reversibly arrests meiosis during in vitro maturation of porcine oocytes.
Jang WI, et al. Anim Reprod Sci. 2014 Jan 30;144(3-4):102-8. PMID: 24374180.
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