CPUY074020 是一种高效、有口服活性的组蛋白甲基转移酶 G9a 抑制剂,其 IC50 值为 2.18 μM。CPUY074020 具有抗增殖活性。
产品描述
CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
体外活性
CPUY074020 (2.5-10μM ; 48 hours) dose-dependently de-regulates H3K9 trimethylation. CPUY074020 (2-8μM; 24 hours) induces cell death through apoptosis[1].
体内活性
CPUY074020 shows reasonable PK properties, with a T1/2 value of 4.0 hours and an oral bioavailability of 55.5% at an oral dose of 10 mg/kg[1].
Cas No.
902279-44-1
分子式
C25H28N4O2
分子量
416.52
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years