1. Protein Tyrosine Kinase/RTK
  2. Btk

Spebrutinib (Synonyms: AVL-292; CC-292)

Cat. No.: HY-18012 Purity: 99.95%
Handling Instructions

Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.

For research use only. We do not sell to patients.

Spebrutinib Chemical Structure

Spebrutinib Chemical Structure

CAS No. : 1202757-89-8

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10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 312 In-stock
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100 mg USD 504 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Other Forms of Spebrutinib:

    Spebrutinib purchased from MCE. Usage Cited in: Blood. 2016 Jun 23;127(25):3237-52.

    Ibrutinib binds to the ATP-binding pocketof HCK and blocks ATP binding. Results from kinase active-site inhibition assaysutilizing an ATP-BTN probe that is used to pull downactive kinases in the presence of Ibrutinib, CC-292, or A419259 in lysates from BCWM.1 WM cells.
    • Biological Activity

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    • Technical Information

    • Purity & Documentation

    • References

    Description

    Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM.

    IC50 & Target

    IC50: <0.5 nM (Btk)[1]

    In Vitro

    Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC50 value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC50 of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC50=6 nM) correlated directly with the cellular EC50 of Btk kinase inhibition with Spebrutinib (EC50=8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM[1].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 45 mg/mL (106.27 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3616 mL 11.8080 mL 23.6161 mL
    5 mM 0.4723 mL 2.3616 mL 4.7232 mL
    10 mM 0.2362 mL 1.1808 mL 2.3616 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    Cells are incubated in serum-free RPMI media for 1-1.5 hours. Isolated human B cells are incubated with Spebrutinib at a final concentration of 0.001, 0.01, 0.1 and 1 μM. Ramos cells are incubated with 0.1 nM-3 μM Spebrutinib. Cells are then incubated in the presence of compound for 1 hour at 37°C. Following incubation, cells are centrifuged and resuspended in 100 μL of serum-free RPMI and BCR is stimulated with addition of 5 μg/mL α-human IgM. Samples are centrifuged, washed in phosphate-buffered saline (PBS), and lysed in 100 μL of Cell Extraction Buffer plus 1:10 (v/v) PhosSTOP Phosphatase Inhibitor and 1:10 (v/v) Complete Protease Inhibitor. Antibodies used for immunoblot analysis include P-PLCγ2, PLCγ2 (3871; CST), Syk (2712; CST), P-Syk (2710; CST), Btk, P-Btk, and Tubulin. Membranes are scanned on a Li-Cor Odyssey scanner using infrared fluorescence detection[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    423.44

    Formula

    C₂₂H₂₂FN₅O₃

    CAS No.

    1202757-89-8

    SMILES

    COCCOC1=CC=C(NC2=NC=C(F)C(NC3=CC=CC(NC(C=C)=O)=C3)=N2)C=C1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.95%

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    Product Name:
    Spebrutinib
    Cat. No.:
    HY-18012
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    Spebrutinib

    Cat. No.: HY-18012