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    Spebrutinib (CC292; AVL292)
    Spebrutinib (CC292; AVL292)

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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 #: V0644
    CAS #: 1202757-89-8Purity ≥98%

    Description: Spebrutinib (formerly AVL-292; CC-292; SBT) is a covalent/irreversible, orally bioactive, and highly selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase/BTK inhibitor with potential antitumor activity. It inhibits BTK with an IC50 of<0.5 nM, and exhibits > 1400-fold higher selectivity for BTK over the other kinases. 

    References: J Pharmacol Exp Ther. 2013 Aug;346(2):219-28; Br J Haematol. 2013 Nov;163(4):436-43. 

    Related CAS #: 1360053-81-1 (Spebrutinib besylate)

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    • 香港大学
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    Molecular Weight (MW)423.44
    FormulaC22H22FN5O3
    CAS No.1202757-89-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 85 mg/mL (200.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: N-(3-((5-fluoro-2-((4-(2-methoxyethoxy)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide

    InChi Key: KXBDTLQSDKGAEB-UHFFFAOYSA-N

    InChi Code: InChI=1S/C22H22FN5O3/c1-3-20(29)25-16-5-4-6-17(13-16)26-21-19(23)14-24-22(28-21)27-15-7-9-18(10-8-15)31-12-11-30-2/h3-10,13-14H,1,11-12H2,2H3,(H,25,29)(H2,24,26,27,28)

    SMILES Code: C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(OCCOC)C=C3)=NC=C2F)=C1)=O

    SynonymsSpebrutinib; CC-292; AVL292; AVL-292; CC292; CC 292; AVL 292; 


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    In Vitro

    In vitro activity: AVL-292 exhibits dose-dependent inhibition of Btk with EC50 of 8 nM and downstream BCR signaling components in Ramos cells. AVL-292, by inhibiting BTK activities, further inhibits B cell proliferation with EC50 of 3 nM.


    Kinase Assay: The Omnia continuous read assay is performed essentially as described by the vendor. The assay conditions are: 40 μM ATP (1X KMATP), 10 μM Y5-Sox, and 10 nM BTK enzyme. Briefly, a substrate mix containing 1.13X ATP and the Y5 Sox substrate is first prepared in 1X Omnia Kinase Reaction Buffer (KRB) consisting of 20 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EGTA, 5 mMβ-glycerophosphate, 5% glycerol, and 0.2 mM DTT. For IC50 measurements, 5 μL of enzyme are incubated with serially diluted (3-fold) compounds prepared in 50% DMSO in a Corning (#3574) 384-well, white, non-binding surface microtiter plate at 25°C for 30 min. Kinase reactions are started with the addition of 45 μL of the ATP/Y5 substrate mix and monitored at λex360/λem485 in a Synergy 4 plate reader for 60 minutes. Progress curves from each well are examined for linear reaction kinetics and fit statistics. Initial velocity from each reaction is determined from the slope of a plot of relative fluorescence units versus time and then plotted against inhibitor concentration to estimate IC50 using the Response, Variable Slope model in GraphPad Prism from GraphPad Software.


    Cell Assay: A suspension of resting purified naïve human B cells isolated by negative selection in RPMI is prepared at 0.4–0.5 × 106 cells/ml. Cells are mixed together with α-human IgM (final concentration of 5 μg/ml in each well) and vehicle (dimethyl sulfoxide) or AVL-292 (final concentrations of 0.01, 0.1, 1.0, 10.0, 100.0, or 1000 nM per well) and seeded in a 96-well plate. Cells are incubated for 56 hours in a humidified incubator maintained at 37°C and 5% CO2. 3H-Thymidine is added (final concentration of 1 μCi in each well) and cells are incubated overnight, harvested, and measured for 3H incorporation. Experiments are performed in triplicate.

    In VivoIn a collagen-induced arthritis mouse model, AVL-292 (3-30 mg/kg, p.o.) dose-dependently inhibits the clinical signs of inflammatory disease, including reduction in joint and paw swelling and visible redness of the affected paws.
    Animal modelCollagen-induced arthritis (CIA) mouse model
    Formulation & Dosage3-30 mg/kg; p.o
    References

    J Pharmacol Exp Ther. 2013 Aug;346(2):219-28; Br J Haematol. 2013 Nov;163(4):436-43. 


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

     Clinical activity of CC-292

    CC-292 (AVL-292)

    Btk occupancy and Btk protein resynthesis can be detected in mice in vivo. Mice were treated orally once with 50 mg/kg CC-292 to inhibit all Btk protein. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28. 

    CC-292 (AVL-292)

    CC-292 is efficacious in an established collagen-induced arthritis model. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28. 


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