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    LY2090314
    LY2090314

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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 #: V0223
    CAS #: 603288-22-8Purity ≥98%

    Description: LY2090314 (LY-2090314) is a novel and potent GSK-3 (glycogen synthase kinase-3) inhibitor for GSK-3α/β with potential antitumor activity. It inhibits GSK-3α/β with an IC50 of 1.5 nM/0.9 nM. LY2090314 may also improve the antitumor efficacy of platinum-based chemotherapies.

    References:Brail LH, et al. J Clin Oncol, 2011, 29, abstr 3030.

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    Molecular Weight (MW)

    512.53

    Formula

    C28H25FN6O3

    CAS No.

    603288-22-8

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 100 mg/mL (195.1 mM)

    Water: <1 mg/mL

    Ethanol: 2 mg/mL warmed (3.9 mM)

    SMILES

    O=C(C(C1=CN2C3=C1C=C(F)C=C3CN(C(N4CCCCC4)=O)CC2)=C5C6=CN=C7C=CC=CN76)NC5=O

    Synonyms

    LY 2090314; LY2090314; LY-2090314

    Chemical Name: 3-(9-fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-4-(imidazo[1,2-a]pyridin-3-yl)-1H-pyrrole-2,5-dione

    InChi Key: HRJWTAWVFDCTGO-UHFFFAOYSA-N

    InChi Code: InChI=1S/C28H25FN6O3/c29-18-12-17-15-34(28(38)32-7-3-1-4-8-32)11-10-33-16-20(19(13-18)25(17)33)23-24(27(37)31-26(23)36)21-14-30-22-6-2-5-9-35(21)22/h2,5-6,9,12-14,16H,1,3-4,7-8,10-11,15H2,(H,31,36,37)



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    In Vitro

    In vitro activity: LY2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. LY2090314 is able to stabilize β-catenin. LY2090314 shows limited efficacy as monotherapy. LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer cell lines in vitro.

     

    Kinase Assay: LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

     

    Cell Assay: LY2090314 (20 nM) promotes a time-dependent stabilization of β-catenin total protein as well as an induction of Axin2. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases. LY2090314 potently induces apoptotic cell death in a panel of melanoma cell lines irrespective of BRAF mutation status. Cell death induced by LY2090314 is dependent on β-catenin and GSK3β knockdown increases the sensitivity of cells to LY2090314. LY2090314 remains active in cell lines resistant to Vemurafenib and has an independent mechanism of action.

    In Vivo

     LY2090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts

    Animal model

    Athymic nude mice:Five million A375 human melanoma cancer cells are injected S.C. in the flank of female 6 to 8 week old athymic nude mice in a 1:1 mixture with matrigel. Mice are monitored daily for palpable tumors. When tumors reach appr 100 mm2 mice are randomized into groups receiving either LY2090314 (25 mg/kg Q3D) or vehicle (20% Captisol/0.01N HCl) via i.v. administration. Tumor volume (measured by calipers) and animal body weight are recorded twice weekly. Tumor volumes are calculated using the formula: (a2 × b)/2 (a being the smaller and b being the larger dimension of the tumor). For combination studies with DTIC (60 mg/kg QD), LY2090314 is dosed at 2.5 mg/kg Q3D and tumor growth monitored.

    Formulation & Dosage

     LY2090314 (25 mg/kg Q3D) or vehicle (dissolved in 20% Captisol/0.01N HCl) via i.v. administration.

    References

    [1] Brail LH, et al. J Clin Oncol, 2011, 29, abstr 3030.


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

    LY2090314

    LY2090314 is a GSK inhibitor which elevated Wnt signaling in melanoma cell lines.

    LY2090314

    LY2090314 potently induces apoptotic cell death in a range of melanoma cell lines irrespective of BRAF mutation status.

    LY2090314

    Cell death induced by LY2090314 is dependent on β-catenin and GSK3β knockdown increases the sensitivity of cells to LY2090314. A. Melanoma cells stably transfected with shRNAs targeting β-catenin display decreased β-catenin and Axin2 protein expression by western blot. A375 (B) and M14 (C) cells expressing shRNAs targeting β-catenin (● Control; ■ β-catenin shRNA 1; ▲ β-catenin shRNA 2; ▼ β-catenin shRNA 3) become resistant to LY2090314 suggesting that β-catenin is required for apoptotic cell death in response to LY2090314. D, E. A375 cells targeted with GSK3β shRNA, but not GSK3α shRNA, demonstrates increased sensitivity to LY2090314 (4.5nM, 72hr).  2015 Apr 27;10(4):e0125028.

    LY2090314

    LY2090314 demonstrates activity in cell lines resistant to the BRAF inhibitor Vemurafenib and has an independent mechanism of action.  2015 Apr 27;10(4):e0125028.

    LY2090314

    LY2090314 elevates Axin2 gene expression in vivo, demonstrates single agent activity in the A375 xenograft model of melanoma and enhances the efficacy of DTIC.  2015 Apr 27;10(4):e0125028.


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