Dinaciclib | CDK inhibitor

Dinaciclib (779353-01-4) is a potent and selective inhibitor of cyclin-dependent kinases CDK1, CDK2, CDK5, and CDK9 (IC₅₀s respectively: 3 nM, 1 nM, 1 nM, and 4 nM).^1,2 Active across multiple human cancer cell lines and in mouse xenograft models.^3-9

References/Citations:

1. Paruch et al. (2010), Discovery of Dinaciclib (SCH 727965): A potent and Selective Inhibitor of Cyclin-Dependent Kinase; ACS Med. Chem. Lett., 1 204
2. Parry et al. (2010), Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor; Mol. Cancer Ther., 9 2344
3. Saqub et al. (2020), Dinaciclib, a cyclin-dependent kinase inhibitor, suppresses cholangiocarcinoma growth by target CDK2/5/9; Sci. Rep., 10 18489
4. Howard et al. (2021), Dinaciclib, a Bimodal Agent Effective against Endometrial Cancer; Cancers (Basel)., 13 1135
5. Buzzetti et al. (2021), Pre-therapeutic efficacy of the CDK inhibitor dinaciclib in medulloblastoma cells; Sci. Rep., 11 5374
6. Nelson et al. (2022), Synthetic lethality of cyclin-dependent kinase inhibitor Dinaciclib with VHL-deficiency allows for selective targeting of clear cell renal carcinoma; Cell Cycle, 21 1103
7. Howard et al. (2022), Dinaciclib as an effective pan-cyclin dependent kinase inhibitor in platinum-resistant ovarian cancer; Front. Oncol., 12 1014280
8. Schott et al. (2024), Osteosarcoma PDX-Derived Cell Line Models for Preclinical Drug Evaluation Demonstrate Metathesis Inhibition by Dinaciclib through a Genome-Targeted Approach; Clin. Cancer Res., 30 849
9. Valdez Capuccino et al. (2024), CDK9 inhibition as an effective therapy for small cell lung cancer; Cell Death Dis., 15 345