Name: Dinaciclib (SCH727965)
Price: 260.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Dinaciclib is a potent cyclin-dependent kinase (CDK) inhibitor with IC50s for CDK2, CDK5, CDK1 and CDK9 at 1 nM, 1 nM, 3 nM, and 4 nM, respectively. [1] It is in phase I or II clinical trials for various cancers.
    Dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. [2] Inhibition of CDK 1 suppresses Rb phosphorylation, leading to cell cycle arrest and apoptosis. [3]
    Dinaciclib is active against a broad spectrum of human tumor cell lines in vitro and in vivo. It has great potential to improve cancer chemotherapy.
    
    [1]Parry D., et al. (2010). Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor. Mol Cancer Ther (9): 2344- 2353.
    [2]Martin, M. P., et al. (2013). Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chemical Biology 8 (11): 2360–5.
    [3]Payton M., et al. (2006). Discovery and Evaluation of Dual CDK1 and CDK2 Inhibitors. Cancer Res 66: 4299-4308.
- Properties
  - Alternative Name
    
    2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol
    
    CAS Number
    
    779353-01-4
    
    Molecular Formula
    
    C21H28N6O2
    
    Molecular Weight
    
    396.49
    
    Appearance
    
    A solid
    
    Purity
    
    99.64%
    
    Solubility
    
    insoluble in H2O; ≥10.22 mg/mL in EtOH; ≥17.15 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Li J, Ji H, et al. "Characterizing CDK8/19 Inhibitors through a NFκB-Dependent Cell-Based Assay." Cells. 2019 Oct 6;8(10). pii: E1208. PMID:31590445
    2. Rello-Varona S, Fuentes-Guirado M, et al. "Bcl-x(L) inhibition enhances Dinaciclib-induced cell death in soft-tissue sarcomas." Sci Rep. 2019 Mar 7;9(1):3816. PMID:30846724
    3. Cing?z O, Goff SP. "Cyclin-dependent kinase activity is required for type I interferon production." Proc Natl Acad Sci U S A. 2018 Mar 27;115(13):E2950-E2959. PMID:29507205

Dinaciclib (SCH727965)

Dinaciclib (SCH727965)

Background

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