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Acalabrutinib

CAS No. : 1420477-60-6

MCE 国际站：Acalabrutinib

产品活性：Acalabrutinib (ACP-196) 是一种具有口服活性，不可逆的，高度选择性的第二代 BTK 抑制剂。Acalabrutinib 与 BTK 的 ATP 结合口袋中的 Cys481 共价结合。Acalabrutinib 在慢性淋巴细胞性白血病 (CLL) 小鼠模型中显示出强大的靶向作用和功效。Acalabrutinib 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells. In the human CLL NSG xenograft model, Acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferation.
Acalabrutinib inhibits purified BTK with an IC₅₀ of 3 nM and an EC₅₀ of 8 nM in a human whole-blood CD69 B cell activation assay. Acalabrutinib has improved target specificity over ibrutinib with 323-, 94-, 19-, and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC , respectively) and no activity against EGFR.

In Vivo: Acalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activity.

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