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    Abemaciclib (LY2835219)
    Abemaciclib (LY2835219)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V3692
    CAS #: 1231929-97-7 Purity ≥98%

    Description: Abemaciclib (formerly known as LY2835219; trade name: Verzenio) is a potent and selective, and orally bioavailable dual  inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. In September 2017, Abemaciclib was approved by FDA to treat certain advanced or metastatic breast cancers. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6 can cause cell cycle deregulation as seen in certain types of cancer.

    References:  2016 Mar 22;7(12):14803-13;  2017 Jan 15;124:29-42.

    Related CAS#1231929-97-7 (free base)1231930-82-7 (mesylate salt)

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    Molecular Weight (MW)506.59
    FormulaC27H32F2N8
    CAS No.1231930-82-7 (mesylate); 1231929-97-7 (free base);  
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >10 mM
    Water: N/A
    Ethanol: N/A
    SMILES CodeCC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C
    SynonymsAbemaciclib; LY2835219; LY-2835219; LY 2835219; Abemaciclib methanesulfonate; LY2835219 methanesulfonate


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    In Vitro

    In vitro activity: Abemaciclib (formerly known as LY2835219) is a potent and selective, orally available dual  inhibitor of CDK4 (cyclin-dependent kinase) and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6 can cause cell cycle deregulation as seen in certain types of cancer. 


    Kinase Assay: Cells (5 × 103) are plated in 96 well plates. Cells are treated the next day for 24 to 48 hours and then assessed for caspase-3 activity by Caspase-Glo-3/7 Assay, as per manufacturer's instructions and a luminescence plate reader.


    Cell Assay: Cells are seeded in a 96-well plate, allowed to adhere overnight, and treated with DMSO control (0.1% v/v) or the indicated compounds for 72 h. Cell viability and proliferation are determined using a Cell Counting Kit according to the manufacturer's instructions. The interaction between LY2835219 and mTOR inhibitor is determined using CompuSyn. Combination index (CI) values of 1 indicates and additive drug interaction, whereas a CI of < 1 is synergistic and a CI of > 1 is antagonistic.

    In VivoLY2835219 saturates BBB efflux with an unbound plasma IC50 of about 95 nM. The percent of dose in brain for LY2835219-MsOH is 0.5–3.9%. In both a subcutaneous and intracranial human glioblastoma model (U87MG), LY2835219-MsOH suppressed tumor growth in a dose-dependent manner both as a single agent, and in combination with temozolomide. 
    Animal modelBALB/c female nude mice are injected subcutaneously with OSC-19 (1×106) cells
    Formulation & DosageDissolved in 1% HEC in 20 mM phosphate buffer (pH2.0); 45 mg/kg/d or 90 mg/kg/d)
    References 2016 Mar 22;7(12):14803-13;  2017 Jan 15;124:29-42; 2011 Nov 12-16; San Francisco, CA. Philadelphia (PA): AACR; Mol Cancer Ther 2011;10(11 Suppl):Abstract B234. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Abemaciclib (LY2835219)


    Effects of LY2835219 on RB pathway and intracellular signaling.  2016 Mar 22;7(12):14803-13.

     Abemaciclib (LY2835219)


    Combined effect of LY2835219 and mTOR inhibitors in vitro.  2016 Mar 22;7(12):14803-13.

     Abemaciclib (LY2835219)


    LY2835219 and mTOR inhibitor combination in HNSCC xenograft tumor model.  2016 Mar 22;7(12):14803-13.

     Abemaciclib (LY2835219)


    Antitumor activity of LY2835219 in HNSCC xenograft tumor model.  2016 Mar 22;7(12):14803-13.

     Abemaciclib (LY2835219)


    Effects of CDK4/6 inhibitor LY2835219 on cell growth in HNSCC.  2016 Mar 22;7(12):14803-13.

     Abemaciclib (LY2835219)


    Effects of LY2835219 on cell proliferation and cell cycle in HNSCC.  2016 Mar 22;7(12):14803-13.


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