Name: Cdk4/6 Inhibitor IV
Price: 361.00 USD

- Overview
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    Background
    
    Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine inhibitor for Cdk4/cyclin D1 and Cdk6/cyclin D1 [1]. Cyclin-dependent kinase 4 (Cdk4) is an important cell cycle kinase, since its activity is required for initiating the phosphorylation of the retinoblastoma protein (pRb). Hyperphosphorylation of pRb prevents cells from initiating DNA synthesis, releases the sequestered transcription factors, leading to the loss of pRb's growth-inhibitory function, thus allowing cells to enter S phase [1]. In vitro: Cdk4/6 inhibitor IV showed an inhibitory effect on Cdk4/cyclin D1 and Cdk6/cyclin D1with the IC50 values of 1.5 and 5.6 μM, respectively. Cdk4/6 inhibitor IV exihibited potent selectivity for Cdk4/6 over Cdk5/p35, c-met, v-abl, IGF-1R, insulin receptor, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D2, Cdk6/cyclin D2, and Cdk1/cyclin B with the IC50 values ≥ 10-100 μM. In asynchronous cell lines, at 5-10 μM, Cdk4/6 inhibitor IV blocked retinoblastoma protein phosphorylation at Ser780 and Ser795, inducing cell cycle arrest in the G1 phase and apoptosis. In vivo: In mice xenografted with human HCT116 colon carcinoma, treatment with of Cdk4/6 inhibitor IV (i.p, 30 mg/kg) after 29 days suppressed tumor growth.
- Properties
  - Alternative Name
    
    CINK4; trans-4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-cyclohexanol
    
    CAS Number
    
    359886-84-3
    
    Molecular Formula
    
    C27H32N6O
    
    Molecular Weight
    
    456.6
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤1mg/ml in ethanol;30mg/ml in DMSO;20mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only