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    Glasdegib Maleate (PF04449913)
    Glasdegib Maleate (PF04449913)

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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 #: V21617
    CAS #: 2030410-25-2Purity ≥98%

    Description: Glasdegib Maleate (formerly known as PF-04449913), the Maleate salt of glasdegib, is a novel potent, and orally bioavailable small-molecule inhibitor of Smoothened (Smo) in the Hedgehog (Hh) signaling pathway with IC50 of 5 nM. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of cancers. Glasdegib significantly reduces medulloblastoma growth in a Ptch1+/-p53+/- allograft model at doses that decreased murine Shh target gene expression. In stromal co-culture experiments, FACS analysis demonstrates a significant reduction in BC LSC by PF-04449913 when compared with normal progenitors.

    References: ACS Med Chem Lett. 2011 Dec 21;3(2):106-11.

    Related CAS#2030410-25-2 (Maleate)1095173-27-5 (free base); 1095173-64-0 (HCl); 1352568-48-9 (2HCl)    

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    Molecular Formula: C25H26N6O5; 

    Molecular Weight: 490.52
    Related CAS #: 1095173-27-5 (free base)     1095173-64-0 (HCl)   2030410-25-2 (maleate)     1352568-48-9 (2HCl)                                         

    Synonym: PF913 maleate; PF 04449913 maleate; PF 913 maleate; PF04449913 maleate; PF-913 maleate; PF-04449913 maleate 

    Chemical Name: 1-((2R,4R)-2-(1H-Benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate

    InChi Key: VJCVKWFBWAVYOC-UIXXXISESA-N

    InChi Code: InChI=1S/C21H22N6O.C4H4O4/c1-27-11-10-16(24-21(28)23-15-8-6-14(13-22)7-9-15)12-19(27)20-25-17-4-2-3-5-18(17)26-20;5-3(6)1-2-4(7)8/h2-9,16,19H,10-12H2,1H3,(H,25,26)(H2,23,24,28);1-2H,(H,5,6)(H,7,8)/b;2-1-/t16-,19-;/m1./s1

    SMILES Code: O=C(NC1=CC=C(C#N)C=C1)N[[email protected]]2C[[email protected]](C3=NC4=CC=CC=C4N3)N(C)CC2.O=C(O)/C=C\C(O)=O           


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    In Vitro

    In vitro activity: In vitro microsomal assays, PF-04449913 have high clearance in rat and low clearance in dog and human, without inhibiting any of the major cytochrome P450 isoforms. 


    Kinase Assay: Glasdegib (formerly known as PF-04449913) is a novel potent, and orally bioavailable small-molecule inhibitor of Smoothened (Smo) in the Hedgehog (Hh) signaling pathway with IC50 of 5 nM. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of cancers. Glasdegib significantly reduces medulloblastoma growth in a Ptch1+/-p53+/- allograft model at doses that decreased murine Shh target gene expression. In stromal co-culture experiments, FACS analysis demonstrates a significant reduction in BC LSC by PF-04449913 when compared with normal progenitors.


    Cell Assay: In the Hedgehog (Hh) signaling pathway, the combination of Hh ligands and their receptor Patched leads to the activation of smoothened and subsequently activation of three transcription factors Gli1, Gli2 and Gli3. It then leads to the proliferation of cells. As an antagonist of smoothened, PF-04449913 is developed for treatment of cancer.

    In VivoIn rat and dog, PF-04449913 shows high clearance, and good oral bioavailability
    Animal modelRat, dog
    Formulation & DosageDissolved in 10% EtOH/20% PEG400/70% PBS (i.v.); 0.5% methylcellulose in water (p.o.); 1 mg/kg (Rat); 0.5 mg/kg (dog i.v.); 3 mg/kg (dog p.o.); i.v. or p.o. administration
    ReferencesACS Med Chem Lett. 2011 Dec 21;3(2):106-11.


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




    Glasdegib (PF-04449913)

    Selective shh inhibition reduces lsc burden in stromal co-cultures.  2015 Mar 21;13:98. 

     

    Glasdegib (PF-04449913)

    Shh inhibition induces cycling of dormant leukemic progenitors.  2015 Mar 21;13:98. 

     

    Glasdegib (PF-04449913)

    PF-04449913 induced cell cycle activation enhances TKI sensitivity.  2015 Mar 21;13:98. 

     

    Glasdegib (PF-04449913)

    GLI2 induces cell cycle arrest in leukemic progenitors.  2015 Mar 21;13:98. 

     

    Glasdegib (PF-04449913)

    SHH pathway deregulation in chronic myeloid leukemia progression.  2015 Mar 21;13:98. 



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