AZD-5438

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服 CDK1/2/9 抑制剂，IC50 分别为 16/6/20 nM；还在体外抑制 p25-Cdk5 (IC50=14 nM) 和 GSK-3β (IC50=17 nM) 的激酶活性。

A potent and oral inhibitor of CDK1/2/9 with IC50 of 16/6/20 nM, respectively; also inhibits the kinase activity of p25-Cdk5 (IC50=14 nM) and GSK-3β (IC50=17 nM) in vitro, displays 75-fold less active against cyclin D-Cdk4; shows significant antiproliferative activity in human tumor cell lines (IC50 range: 0.2-1.7 uM), inhibits the phosphorylation of Cdk substrates pRb, nucleolin, PP1A, and RNA polymerase II COOH-terminal domain and blocks cell cycle; inhibits the human tumor xenograft growth in vivo; also inhibits PASTA kinase in L. monocytogenes (PrkA) and L. monocytogenes growth in a β-lactam-synergism-dependent manner.Solid Tumors Phase 1 Discontinued.

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AZD 5438 | AZD5438

Cell Cycle/DNA Damage

CDK

CDK1|CDK2|CDK9

Cancer

Solid Tumors

602306-29-6

371.4566

C18H21N5O2S

>98% (HPLC)

10 mM in DMSO

O=S(C1=CC=C(NC2=NC=CC(C3=CN=C(C)N3C(C)C)=N2)C=C1)(C)=O

2-Pyrimidinamine, 4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years