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    MK-4101
    MK-4101

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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 #: V2914
    CAS #: 935273-79-3Purity ≥98%

    Description: MK-4101 is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway. MK-401 has the potential for the treatment of medulloblastoma and BCC (Basal Cell Carcinoma) as it is highly active against these cells. MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line (Gli Luc) with IC50 of 1.5 µM and in human KYSE180 oesophageal cancer cells with an IC50 of 1 µM. Furthermore, MK-4101 displaced a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 µM. MK-4101 arrests cells in G1 and G2 phases. Beside antitumor activity on transplanted tumors, MK-4101 was highly efficacious against primary medulloblastoma and BCC developing in the cerebellum and skin of Ptch1(+/-) mice. 

    References:  2016 Jun;15(6):1177-89. 


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    Molecular Weight (MW) 493.47
    Formula C24H24F5N5O
    CAS No. 935273-79-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 98 mg/mL (198.59 mM) 
    Water: <1 mg/mL
    Ethanol: 60 mg/mL (121.58 mM) 
    SMILES Code FC(C1=CC=CC=C1C2=NN=C(C34CCC(C5=NOC(C6CC(F)(F)C6)=N5)(CC4)CC3)N2C)(F)F
    Synonyms MK-4101; MK 4101; MK4101


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    In Vitro

    In vitro activity: MK-4101 is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway. MK-401 has the potential for the treatment of medulloblastoma and BCC (Basal Cell Carcinoma) as it is highly active against these cells. MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line (Gli Luc) with IC50 of 1.5 µM and in human KYSE180 oesophageal cancer cells with an IC50 of 1 µM. Furthermore, MK-4101 displaced a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 of 1.1 µM. MK-4101 arrests cells in G1 and G2 phases. 


    Kinase Assay: MK-4101 is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway.  


    Cell Assay: BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. 

    In VivoMK-4101 has displayed robust antitumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. MK-4101 is highly efficacious against primary medulloblastoma and basal cell carcinoma(BCC) developing in the cerebellum and skin of Ptch1+/- mice. Pharmacokinetics of MK-4101 shows that it could be administered orally, showing a good bioavailability (F ≥ 87 %) with low-to-moderate plasma clearance in mice and rats. Moreover, it was well absorbed, and mainly excreted into the bile
    Animal model C57bl/6 mice or Sprague-Dawley rats. 
    Formulation & Dosage 0.5% methylcellulose in deionized water. 40 or 80 mg/kg once a day; 80 mg/kg twice a day. oral administration
    References  2016 Jun;15(6):1177-89. 


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

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