General description
一种有效的pan-AKT激酶抑制剂,抑制Akt1、Akt2和Akt3,IC50分另为3nM、8nM和8nM。
AZD5363 is an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AKT inhibitor AZD5363 binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism. A wide range of solid and hematological malignancies show dysregulated PI3K/AKT/mTOR signaling due to mutations in multiple signaling components。
AZD5363是一种可口服的丝氨酸/苏氨酸蛋白激酶AKT(蛋白激酶B)抑制剂,具有潜在的抗肿瘤活性。 AKT抑制剂AZD5363结合并抑制所有AKT亚型。 抑制AKT可阻止介导细胞过程(例如细胞分裂,细胞凋亡以及葡萄糖和脂肪酸代谢)的AKT底物的磷酸化。 由于多种信号成分的突变,多种实体和血液系统恶性肿瘤显示PI3K / AKT / mTOR信号失调。
Properties
Iupac Name: | (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide |
Inchi Code | 1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1 |
Inchi Key | JDUBGYFRJFOXQC-KRWDZBQOSA-N |
安全信息