LY2606368 HCl

- Overview
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    Background
    
    LY2606368 HCl is a selective ATP competitive inhibitor of checkpoint kinase 1(CHK1) with IC50 value of 1.5nM in SW1990 cells [1].
    CHK1 is an intracellular serine/threonine kinase that plays a role in DNA damage response pathway. The inhibitors of CHK1 are developed for the treatment of cancers. LY2606368 HCl is an ATP-competitive inhibitor of CHK1 and is undergoing clinical trials currently. It inhibits the auto-phosphorylation of CHK1 and induces the phosphorylation of H2AX in cancer cells. In the pancreatic cell line SW1990, LY2606368 HCl significantly inhibits cell proliferation with IC50 value of 1.5nM. LY2606368 HCl also exerts potent anti-tumor activity in SW1990 xenograft model. Besides that, in the orthotopic SKVO3 model, treatment of LY2606368 HCl is found to inhibit tumor growth and reduce the incidence of metastases and accumulation. However, LY2606368 HCl is only administered intravenously due to its poor oral bioavailability [1, 2 and 3].
    
    [1] Wu W, Bi C, Bence A K, et al. Antitumor activity of Chk1 inhibitor LY2606368 as a single agent in SW1990 human pancreas orthotopic tumor model. Cancer Research, 2012, 72(8 Supplement): 1776.
    [2] Lainchbury M, Matthews T P, McHardy T, et al. Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. Journal of medicinal chemistry, 2012, 55(22): 10229-10240.
    [3] McNeely S C, Burke T F, DurlandBusbice S, et al. Abstract A108: LY2606368, a second generation Chk1 inhibitor, inhibits growth of ovarian carcinoma xenografts either as monotherapy or in combination with standard-of-care agents. Molecular Cancer Therapeutics, 2011, 10(Supplement 1): A108.
- Properties
  - Alternative Name
    
    5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile hydrochloride
    
    CAS Number
    
    1234015-52-1 (free base)
    
    Molecular Formula
    
    C18H20ClN7O2
    
    Molecular Weight
    
    401.85
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥6.63 mg/mL in DMSO with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

LY2606368 HCl

Background

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