Name: CRT 0066101
Price: 349.00 USD

- Overview
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    Background
    
    IC50: A potent protein kinase D (PKD) antagonist with the IC50 of 1, 2.5 and 2 nM for PKD1, PKD2, PKD3 respectively.CRT 0066101 is a specific inhibitor of all PKD isoforms. Increasingly studies reveals that PKD family members play an important role in regulating several cellular processes and activities, including chromatin organization, Golgi function, gene expression, cell survival, adhesion, motility, differentiation, DNA synthesis and proliferation. By suppressing PKD, CRT 0066101 is supposed to ameliorate symptoms of pancreatic cancer. [1]In vitro: In Panc-1 cell line based assays, CRT0066101 was reported to reduce bromodeoxyuridine incorporation; increase cell apoptosis; suppress neurotensin-induced PKD1/2 activation; block neurotensin-induced Hsp27 phosphorylation; interrupt PKD1-mediated NF-κB activation as well as down-regulate expression of NF-κB-dependent proliferative and pro-survival proteins. [1]In vivo: In Panc-1 subcutaneous xenograft model, orally administration of CRT0066101 at the dosage of 80 mg/kg/d for 24 days significantly suppressed pancreatic cancer growth. Moreover, when CRT0066101 reached its peak concentration (12 μmol/L) in tumor model, the expression of activated PKD1/2 in the treated tumor explants was substantially decreased. It was concluded that CRT0066101 given orally at 80 mg/kg/d for 21 days in Panc-1 orthotropic model suppressed tumor growth potently in vivo. [1]Clinical trial: So far, no clinical trial has been conducted.
- Properties
  - Alternative Name
    
    (R)-2-(4-((2-aminobutyl)amino)pyrimidin-2-yl)-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride
    
    CAS Number
    
    1883545-60-5
    
    Molecular Formula
    
    C18H24Cl2N6O
    
    Molecular Weight
    
    411.33
    
    Appearance
    
    A solid
    
    Purity
    
    98.78%
    
    Solubility
    
    insoluble in H2O; ≥15.65 mg/mL in DMSO; ≥4.49 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CRT 0066101

CRT 0066101

Background

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