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    Taladegib (LY2940680)
    Taladegib (LY2940680)

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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 #: V1334
    CAS #: 1258861-20-9Purity ≥98%

    Description: Taladegib (formerly LY2940680, LY 2940680, LY-2940680) is a potent and orally bioavailable Hedgehog pathway antagonist of the smoothened receptor being developed by Eli Lilly for the treatment of cancer. It acts by binding to the Smoothened (Smo) receptor, thus inhibiting the Hedgehog (Hh) signaling pathway. Taladegib has the potential to be used in patient with cancer who are resistant to vismodegib.

    References: Expert Opin Investig Drugs. 2011 Dec;20(12):1649-64.

    Related CAS#: 1258861-21-0 (HCl)

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    Molecular Weight (MW)512.5
    FormulaC26H24F4N6O
    CAS No.1258861-20-9  (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 5 mg/mL (9.8 mM)
    Water:<1 mg/mL
    Ethanol: 2 mg/mL (3.9 mM)
    Other infoChemical Name: 4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide
    InChi Key: SZBGQDXLNMELTB-UHFFFAOYSA-N
    InChi Code: InChI=1S/C26H24F4N6O/c1-34(25(37)20-8-7-16(27)15-21(20)26(28,29)30)17-10-13-36(14-11-17)24-19-6-4-3-5-18(19)23(32-33-24)22-9-12-31-35(22)2/h3-9,12,15,17H,10-11,13-14H2,1-2H3
    SMILES Code: O=C(N(C)C1CCN(C2=NN=C(C3=CC=NN3C)C4=C2C=CC=C4)CC1)C5=CC=C(F)C=C5C(F)(F)F
    SynonymsLY2940680, LY 2940680, LY-2940680


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    In Vitro

    In vitro activity: LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib.


    Kinase Assay: Taladegib, a small-molecule antagonist of the smoothened receptor, shows a slight inhibitory effect on cell proliferation without differences between mucin- (IC50: Taladegib=49.8±4.5 μM) and mixed- Cholangiocarcinoma (CCA) (IC50: Taladegib=61.2±21.1 μM).


    Cell Assay: When tested with cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib, LY2940680 inhibited cell proliferation.

    In VivoLY2940680 has excellent pharmacokinetic properties in rodent and non-rodent species. LY2940680 administrated orally treats Ptch+/- p53-/- transgenic mice which spontaneously develop medulloblastoma, produces remarkable efficacy and significantly improves their survival. LY2940680 reveals rapid kinetics of anti-tumor activity through magnetic resonance imaging of these mice, and LY2940680 induces Caspase-3 activity and reduces proliferation by immunohistochemistry analysis of medulloblastoma tumors. LY2940680 inhibits Hh regulated gene expression in the subcutaneous xenograft tumor stroma and produces significant anti-tumor activity.
    Animal model Mice
    Formulation & Dosage Oral
    ReferencesExpert Opin Investig Drugs. 2011 Dec;20(12):1649-64.


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

    Taladegib (LY2940680)

    Effect of Sonic Hedgehog (Hg) pathway inhibitors on proliferation and apoptosis of mucin and mixed CCA primary cultures.  2015 Nov 16;10(11):e0142124. 




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