RO-3306
CDK1 inhibitor / RO-3306 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
Biochemicals & reagents
872573-93-8
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
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TARGET: Kinase -- PATHWAY: Cell cycle; Apoptosis inducer -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer