1. Protein Tyrosine Kinase/RTK
  2. Btk

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

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

AVL-292 is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays.

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

AVL-292 Chemical Structure

AVL-292 Chemical Structure

CAS No. : 1202757-89-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 312 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 504 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of AVL-292:

    AVL-292 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.

    AVL-292 purchased from MCE. Usage Cited in: Patent. US20170333436A1.

    FIG shows results from kinase active-site inhibition assays utilizing an ATP-biotin (ATP-BTN) probe that is used to pull-down active kinases in presence of Ibrutinib, CC-292, or A419259 in lysates from BCWM.1 WM cells.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    AVL-292 is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays.

    IC50 & Target

    IC50: <0.5 nM (Btk)[1]

    In Vitro

    AVL-292 (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC50 value of 0.5 nM. AVL-292 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 AVL-292 dose-response in Ramos cells (EC50=6 nM) correlated directly with the cellular EC50 of Btk kinase inhibition with AVL-292 (EC50=8 nM). Furthermore, the concentration at which AVL-292 inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of AVL-292 required for 90% occupancy of Btk is 39 nM[1].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [1]

    AVL-292 is run in a kinase selectivity panel at Reaction Biology Corporation using HotSpotSM technology and radioisotope-based P81 filtration. AVL-292 is dissolved in pure DMSO to the final 1 μM test concentration. Substrates for the various kinases tested against AVL-292 are prepared fresh daily in Reaction Buffer. Any required cofactors are then added to substrate solution followed by kinase addition and preincubated for 30 min at room temperature. 33P-ATP (10 μM) is delivered into the reaction mixture to initiate the reaction and continued for 2 hr at room temperature. The reaction is terminated and any unreacted phosphate is washed away using 0.1% phosphoric acid prior to detection utilizing a proprietary technology. The study is performed in duplicate and 10 μM staurosporine, a non-selective, ATP-competitive kinase inhibitor, is used as the positive control[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    AVL-292 (CC-292) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    Cells are incubated in serum-free RPMI media for 1-1.5 hours. Isolated human B cells are incubated with AVL-292 at a final concentration of 0.001, 0.01, 0.1 and 1 μM. Ramos cells are incubated with 0.1 nM-3 μM AVL-292. 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

    Solvent & Solubility

    DMSO: ≥ 45 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.95%

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    Inquiry Information

    Product Name:
    AVL-292
    Cat. No.:
    HY-18012
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