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    R428 (BGB-324; R-428)
    R428 (BGB-324; R-428)

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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 #: V0635
    CAS #: 1037624-75-1Purity ≥98%

    Description: Bemcentinib (formerly known as BGB324; R428) is a novel, potent and selective inhibitor of the RTK (receptor tyrosine kinase) Axl with potential anticancer activity. It inhibits Axl with an IC50 of 14 nM, and shows >100-fold higher selectivity for Axl over Abl. R428 showed high activity in blocking tumor spread and prolonging survival in animal models with metastatic breast cancer. Axl signaling regulates breast cancer metastasis at multiple levels in tumor cells and tumor stromal cells and that selective Axl blockade by R428 confers therapeutic value in prolonging survival of animals bearing metastatic tumors. 

    References: Cancer Res. 2010 Feb 15;70(4):1544-54; Blood. 2011 Feb 10;117(6):1928-37. 

    Related CAS: 1037624-91-1 (racemic); 1037624-75-1;   

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    Molecular Weight (MW)506.64
    FormulaC30H34N8
    CAS No.1037624-75-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 6 mg/mL (11.8 mM)          
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)5% DMSO+corn oil: 1 mg/mL
    Chemical Name

    (S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine

    Exact Mass: 506.29064  

    SMILES CodeNC1=NC(NC2=CC=C3C(CC[[email protected]@H](N4CCCC4)CC3)=C2)=NN1C5=NN=C6C(CCCC7=CC=CC=C76)=C5
    SynonymsBGB-324; R428; Bemcentinib; R 428; R-428; BGB324; BGB 324;  


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    In Vitro

    In vitro activity: R428 (also known as BGB324) blocks the catalytic and pro-cancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. In a recent study, the Axl inhibitor R428 shows a mean IC50 dose of ∼ 2.0μM for the primary CLL B cells after 24 hours of treatment and normal B-, T-, and natural killer (NK) cells show no significant amount of cell death at this dose of R428 (2.5 μM) under similar experimental conditions.


    Kinase Assay:  R428 (also known as BGB324) is a potent and selective inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. The selectivty of R428 for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective). A five-point R428 dose titration was performed in radiometric in vitro kinase assays on 133 kinases at the KmATP for each kinase. Axl, Mer, and Tyro3 (Carna Biosciences) assays were also performed using a fluorescence polarization protocol. HER2 activity was determined by Z'-LYTE assay.


    Cell Assay: HeLa cells were seeded in starvation medium in 96-well plates. Twenty-four hours later, cells were preincubated for 1 h with diluted R428 before stimulation with preclustered anti-Axl antibody. Cells were fixed, blocked, and stained with anti–phospho-Akt (Ser473) followed by goat anti-rabbit horseradish peroxidase before developing using SuperSignal ELISA Pico chemiluminescent substrate.

    In VivoPharmacologic investigations reveal favorable exposure after oral administration such that R428-treated tumors display a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibits angiogenesis in corneal micropocket and tumor models. R428 administration reduces metastatic burden and extends survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis.
    Animal modelMDA-MB-231-luc-D3H2LN Intracardiac Model
    Formulation & DosageDissolved in 0.5% hydroxypropylmethylcellulose + 0.1% Tween 80; 125 mg/kg; Oral gavage
    ReferencesCancer Res. 2010 Feb 15;70(4):1544-54; Blood. 2011 Feb 10;117(6):1928-37. 


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

    R428 (BGB324)

    R428 (BGB324)
    R428 (BGB324)

    R428 (BGB324)

    A, experimental protocol for MDA-MB-231-luc-D3H2LN metastasis prevention study.  2010 Feb 15;70(4):1544-54.

    R428 (BGB324)

    A, experimental protocol for 4T1 orthotopic metastasis study.  2010 Feb 15;70(4):1544-54.

    R428 (BGB324)

    R428 modulates expression of Snail and GM-CSF in 4T1 primary tumors.  2010 Feb 15;70(4):1544-54.


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