2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. Spebrutinib besylate

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

目录号: HY-18012A
产品使用指南

摩尔计算器

Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) 是共价，高选择性和口服活性的 Btk 抑制剂，IC50 为0.5 nM。

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Spebrutinib besylate Chemical Structure

Spebrutinib besylate Chemical Structure

CAS No. : 1360053-81-1

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Spebrutinib besylate 的其他形式现货产品:

Other Forms of Spebrutinib besylate:

Spebrutinib besylate 相关抗体

Top Publications Citing Use of Products

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

    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.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) 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]
    体外研究
    (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].

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

    Spebrutinib besylate 相关抗体:
    Clinical Trial
    分子量

    581.62

    Formula

    C28H28FN5O6S
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献
    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.
    参考文献

    Spebrutinib besylate 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Spebrutinib besylate1360053-81-1AVL-292CC-292 besylateAVL292AVL 292BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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