General description
一种BTK抑制剂,具有潜在的抗肿瘤活性。
Acalabrutinib is an orally available inhibitor of Bruton’s tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival。
Acalabrutinib是口服的Bruton酪氨酸激酶(BTK)抑制剂,具有潜在的抗肿瘤活性。 给药后,ACP-196抑制BTK的活性并阻止B细胞抗原受体(BCR)信号传导途径的激活。 这样既可以防止B细胞激活,也可以防止BTK介导的下游生存途径激活。 这导致过度表达BTK的恶性B细胞的生长受到抑制。 BTK是src相关BTK / Tec胞质酪氨酸激酶家族的成员,在B细胞恶性肿瘤中过表达。 它在B淋巴细胞的发育,活化,信号传导,增殖和存活中起着重要作用。
Properties
Iupac Name: | (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide |
Inchi Code | 1S/C26H23N7O2/c1-2-6-21(34)32-15-5-7-19(32)25-31-22(23-24(27)29-14-16-33(23)25)17-9-11-18(12-10-17)26(35)30-20-8-3-4-13-28-20/h3-4,8-14,16,19H,5,7,15H2,1H3,(H2,27,29)(H,28,30,35)/t19-/m0/s1 |
Inchi Key | WDENQIQQYWYTPO-IBGZPJMESA-N |
安全信息