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    LXR623
    LXR623

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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 #: V2912
    CAS #: 875787-07-8Purity ≥98%

    Description: LXR623 (formerly known as WAY-252623) is a novel, potent, clinically viable, highly brain-penetrant, highly selective and orally bioavailable synthetic modulator of LXR (Liver X receptor), it is a partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively. As a LXRα-partial/LXRβ-full agonist, LXR623 selectively kills GBM cells in an LXRβ- and cholesterol-dependent fashion, causing tumor regression and prolonged survival in mouse models. LXR623 displayed high efficacy in reducing lesion progression in the murine LDLR(-/-) atherosclerosis model with no associated increase in hepatic lipogenesis either in this model or Syrian hamsters. LXR-623 potently kills U87EGFRvIII and GBM39 cells in vitro while completely sparing NHAs. LXR-623 also increases ABCA1 protein and decreases LDLR protein levels in all three cell lines.

    References:  2016 Nov 14;30(5):683-693.


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    Molecular Weight (MW) 422.78 
    Formula C21H12ClF5N2                 
    CAS No. 875787-07-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: ≥ 47 mg/mL
    Water: <1 mg/mL
    Ethanol: N/A
    Solubility (In vivo)Chemical Name: 2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole
    InChi Key: KYWWJENKIMRJBI-UHFFFAOYSA-N
    InChi Code: InChI=1S/C21H12ClF5N2/c22-18-10-15(24)9-6-13(18)11-29-20(12-4-7-14(23)8-5-12)16-2-1-3-17(19(16)28-29)21(25,26)27/h1-10H,11H2
    SMILES Code: FC(C1=CC=CC2=C(C3=CC=C(F)C=C3)N(CC4=CC=C(F)C=C4Cl)N=C12)(F)F 
    SynonymsLXR623; LXR-623; LXR 623; WAY252623; WAY-252623; WAY 252623. 


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    In Vitro

    In vitro activity: LXR623 (formerly known as WAY-252623) is a  clinically viable, highly brain-penetrant, highly selective and orally bioavailable synthetic modulator of LXR (Liver X receptor). As a LXRα-partial/LXRβ-full agonist, LXR623 selectively kills GBM cells in an LXRβ- and cholesterol-dependent fashion, causing tumor regression and prolonged survival in mouse models. LXR623 displayed high efficacy in reducing lesion progression in the murine LDLR(-/-) atherosclerosis model with no associated increase in hepatic lipogenesis either in this model or Syrian hamsters. LXR-623 potently kills U87EGFRvIII and GBM39 cells in vitro while completely sparing NHAs. LXR-623 also increases ABCA1 protein and decreases LDLR protein levels in all three cell lines. 


    Kinase Assay: LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.


    Cell Assay: LXR-623 treatment of human PBMC in vitro significantly increases transcription of ABCA1 and ABCG1. LXR-623 potently kills U87EGFRvIII and GBM39 cells in vitro while completely sparing NHAs. LXR-623 also increases ABCA1 protein and decreases LDLR protein levels in all three cell lines. LXR-623 suppresses LDLR expression, increases expression of the ABCA1 efflux transporter, and induces substantial cell death in all of the GBM samples tested. LXR-623 (5 μM) also induces GBM cell death through activation of LXRβ.

    In VivoLXR-623 (400 mg/kg, p.o.) crosses the blood-brain barrier, induces target gene expression, and achieves therapeutic levels in GBM cells in the brain with minimal activity in the periphery. LXR-623 inhibits tumor growth, promotes tumor cell death, and prolongs the survival of mice bearing intracranial patient-derived GBMs. LXR-623 (1.5, 5 mg/kg/day) significantly reduces progression of atherosclerosis in animals compared with the placebo group. LXR-623 (50 mg/kg) induces gene expression in rodent peripheral blood cells in rat. LXR-623 (0, 15 and 50 mg/kg) dose-dependently upregulates transcription of ABCA1 and ABCG1 in monkey whole blood cells proportional to dose
    Animal modelFive-week-old female athymic nu/nu mice with U87EGFRvIII IRFP720 or GBM39 IRFP720 cells intracranially injected into the mouse brain. 
    Formulation & DosageDissolved in 0.5% methylcellulose, 2% Tween 80 in water; 400 mg/kg; Oral gavage
    References  2016 Nov 14;30(5):683-693;  2012 Jan;33(2):264-73;  2008 Oct 16;6:59;  2009 Dec;50(12):2358-70.


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

    LXR-623 crosses the blood brain barrier, induces target gene expression, and achieves therapeutic levels in GBM cells in the brain with minimal activity in the periphery.  2016 Nov 14;30(5):683-693.

     LXR623


    LXR-623 kills GBM cells through activation of LXRβ, the dominant subtype in brain tumors.  2016 Nov 14;30(5):683-693.

     LXR623


    LXR-623 inhibits tumor growth, promotes tumor cell death and prolongs the survival of mice bearing intracranial patient-derived GBMs.  2016 Nov 14;30(5):683-693.


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