Ro 3306

RO-3306 (872573-93-8) is a selective inhibitor of CDK1 (IC50?= 35 nM versus CDK2 IC50?= 340nM).1,2?It induces G2/M phase cell cycle arrest and apoptosis. Inhibition of CDK1 with RO-3306 has been shown to have synergistic effects with PARP inhibitors in treating various breast cancers.3,4?It has also been demonstrated to overcome apoptotic resistance in BRAFV600E?human colorectal cancer cells.5

RO-3306 is an ATP-competitive and selective CDK1 inhibitor used against a diverse panel of human kinases. Used in the treatment of malignant tumors in conjunction with PARP inhibitors.

RO-3306 has been used:

• To study the significance of CA4-mediated cytotoxicity in mitotic arrest
• In cell cycle synchronization to conduct a study on proteomics
• As a CDK1 inhibitor, to prevent early mitotic entry

RO-3306 is a selective ATP-competitive inhibitor of CDK1. It inhibites CDK1 cyclin B1 activity with Ki of 35 nM, nearly 10-fold selectivity relative to CDK2/cyclin E and over 50-fold relative to CDK4/cyclin D. RO-3306 has been used to cause cell cycle arrest at the G2/M boundary.

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1) Vassilev?et al.?(2006),?Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1; Proc. Nat. Acad. Sci. USA?103?10660 2) Krasinska?et al.?(2008),?Selective chemical inhibition as a tool to study Cdk1 and Cdk2 functions in the cell cycle; Cell Cycle?7?1702 3) Pierce?et al.?(2013),?Comparative antiproliferative effects of iniparib and olaparib on a panel of triple-negative and non-triple-negative breast cancer cell lines; Cancer Biol. Ther.?14?537 4) Xia?et al.?(2014),?The CDK1 inhibitor RO3306 improves the response of BRCA-proficient breast cancer cells to PARP inhibition;?Int. J. Oncol.?44?735 5) Zhang?et al.?(2018),?Targeting CDK1 and MEK/ERK Overcomes Apoptotic Resistance in BRAF-Mutant Human Colorectal Cancer; Mol. Cancer Res.?16?378