My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    Taladegib (LY2940680)
    Taladegib (LY2940680)

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    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)

    Customer Validation
    Top Publications Citing Invivochem Products
    • Citation of InvivoChem Vorinostat (V0255) by Nature 2021, 597(7874):119-125
    • Citation of InvivoChem Larotrectinib (V2599) by Cell. 2020 Nov 25;183(5):1202-1218.e25
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022: 8, eabm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3
    • Citation of InvivoChem Larotrectinib (V2599) by Cell 2020, doi: 10.1016/j.cell.2020.10.016.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, doi: 10.1126/sciadv.abm9427.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem Vitrakvi by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem APR-246 by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem LOXO-101 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem Eprenetapopt by Science Adv 2022, PMID: 36103522.
    • Citation of InvivoChem Vorinostat/SAHA (V0255) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem  ARRY-470 by Cell 2020, PMID: 33142117 PMCID: PMC8100789
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, PMID: 34433969
    • Citation of InvivoChem BMH-21 (V1435) by Cell Stem Cell 2020, 26(6): 845-861.e12.
    • Citation of InvivoChem Eprenetapopt (APR-246) by Science Adv 2022, doi: 10.1126/sciadv.abm9427.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem V33339 Lys-SMCC-DM1 by PNAS Nexus 2022, pgac063, https://academic.oup.com/pna
    • Citation of InvivoChem 5-azacytidine by Nature 2021, PMID: 34433969
    • Citation of InvivoChem Ruxolitinib/Filgotinib/BMS-911543/Decernotinib by J Allergy Clin Immunol 2020
    • Citation of InvivoChem LGK974 /WNT974 (V1353) by  Cancer Cell 2021 Apr 12;39(4):529-547.e7.
    • Citation of InvivoChem V1386 Napabucasin (BBI-608) by J Exp Clin Cancer Res 2021 Oct 13;40(1):319.
    • Citation of InvivoChem 5-azacytidine (V0404) by Nature 2021, DOI: 10.1038/s41586-021-03850-3.
    • Citation of InvivoChem Epacadostat/INCB024360 (V0942) by Cancer Discov 2022: 12(4):1106-1127.
    • Citation of InvivoChem S63845 (V2797) by Cell Death and Disease 2020, 11:316.
    • Citation of InvivoChem BMS-582949 (V2668) by Cells 2020, 9(6):1472.
    • Citation of InvivoChem Apiin (V4467) by J Med Chem 2020, 63(15):8338-8358.
    • Citation of InvivoChem V0001 venetoclax by WO2021231323A1
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    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


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    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. 




    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?