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Usage

Uses

Used in Oncology:
Ro 3306 is used as an anticancer agent for the treatment of malignant tumors, particularly in conjunction with PARP inhibitors. It is effective against a diverse panel of human kinases and has been demonstrated to have synergistic effects in treating various breast cancers.
Used in Cell Cycle Research:
Ro 3306 is used as a CDK1 inhibitor to prevent early mitotic entry and induce G2/M phase cell cycle arrest. This makes it a valuable tool for studying the significance of CA4-mediated cytotoxicity in mitotic arrest and for conducting proteomics studies on cell cycle synchronization.
Used in Drug Development:
Ro 3306 serves as a lead compound in the development of novel therapeutic agents targeting CDK1. Its selective inhibition of CDK1 and ability to overcome apoptotic resistance in certain cancer cells make it a promising candidate for further research and potential clinical applications.

Biochem/physiol Actions

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.

References

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