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    LY2874455
    LY2874455

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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 #: V0499
    CAS #: 1254473-64-7Purity ≥98%

    Description: LY2874455 (LY-2874455; LY 2874455) is a novel and highly potent pan-FGFR inhibitor with potential anticancer activity. It inhibits FGFR1, FGFR2, FGFR3, and FGFR4 with IC50 values of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM, respectively. It also inhibits VEGFR2 activity with an IC50 of 7 nM. LY2874455 exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines. It shows an excellent broad spectrum of antitumor activity in several tumor xenograft models representing the major FGF/FGFR relevant tumor histologies including lung, gastric, and bladder cancers and multiple myeloma, and with a well-defined pharmacokinetic/pharmacodynamic relationship.

    References: Mol Cancer Ther. 2011 Nov;10(11):2200-10.

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    Molecular Weight (MW)444.31
    FormulaC21H19Cl2N5O2
    CAS No.1254473-64-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 88 mg/mL (198.1 mM)
    Water:<1 mg/mL
    Ethanol: 57 mg/mL (128.3 mM)
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL
    SynonymsLY 2874455; LY-2874455; LY2874455 

    Chemical Name: (R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol.

    InChi Key: GKJCVYLDJWTWQU-CXLRFSCWSA-N

    InChi Code: InChI=1S/C21H19Cl2N5O2/c1-13(21-17(22)10-24-11-18(21)23)30-15-3-5-20-16(8-15)19(26-27-20)4-2-14-9-25-28(12-14)6-7-29/h2-5,8-13,29H,6-7H2,1H3,(H,26,27)/b4-2+/t13-/m1/s1

    SMILES Code: C[[email protected]](C1=C(Cl)C=NC=C1Cl)OC2=CC3=C(NN=C3/C=C/C4=CN(CCO)N=C4)C=C2


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    In Vitro

    In vitro activity: In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and KATO-III cells.


    Kinase Assay: Biochemical filter-binding assays for detection of FGFR phosphorylation activities; Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader.


    Cell Assay: Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS).

    In VivoLY2874455 exhibits a potent inhibition of FGF-induced Erk phosphorylation in the heart tissues of mice with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results in dose-dependent inhibition of the tumor growth.
    Animal modelMice xenograft bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460
    Formulation & Dosage Dissolved in 10% Acacia; 3 mg/kg; p.o.
    References

    Mol Cancer Ther. 2011 Nov;10(11):2200-10.


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

    LY2874455

    Inhibition of FGF/FGFR- and VEGF/VEGFR2-mediated signaling activities in cells by LY2874455. Mol Cancer Ther. 2011 Nov;10(11):2200-10.

    LY2874455

    Effects of LY2874455 on blood pressure in rats. Mol Cancer Ther. 2011 Nov;10(11):2200-10.

    LY2874455

    Efficacy of LY2874455 in different tumor xenograft models. Mol Cancer Ther. 2011 Nov;10(11):2200-10.


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